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Information on EC 3.5.1.98 - histone deacetylase and Organism(s) Homo sapiens and UniProt Accession Q13547

for references in articles please use BRENDA:EC3.5.1.98

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IUBMB Comments

A class of enzymes that remove acetyl groups from N6-acetyl-lysine residues on a histone. The reaction of this enzyme is opposite to that of EC 2.3.1.48, histone acetyltransferase. Histone deacetylases (HDACs) can be organized into three classes, HDAC1, HDAC2 and HDAC3, depending on sequence similarity and domain organization. Histone acetylation plays an important role in regulation of gene expression. In eukaryotes, HDACs play a key role in the regulation of transcription and cell proliferation . May be identical to EC 3.5.1.17, acyl-lysine deacylase.

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
hide
hydrolysis of an N6-acetyl-lysine residue of a histone to yield a deacetylated histone

Synonyms
histone deacetylase, hdac1, hdac6, hdac2, hdac3, hdac4, hdac5, hdac8, hdac9, hdac7, more

SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
class II histone deacetylase
-
histone deacetylase
-
histone deacetylase 1
-
histone deacetylase-1
-
histone deacetylase1
-
acetyl-lysine deacetylase
-
class I acetyl-lysine deacetylase
-
class I histone deacetylase
-
-
class II histone deacetylase
-
class IIa HDAC
-
class IIa histone deacetylase
-
cytoplasmic deacetylase
-
-
HDAC1
HDAC10
-
-
HDAC2
HDAC3
HDAC4
HDAC5
-
-
HDAC6
HDAC6p114
-
splicing variant of histone deacetylase 6 lacking the first 152 amino acids from N-terminus in the major isoform HDAC6p131 protein
HDAC6p131
-
major isoform of histone deacetylase 6
HDAC7
HDAC8
histone deacetylase
histone deacetylase 1
-
-
histone deacetylase 10
-
a class IIb histone deacetylase
histone deacetylase 2
histone deacetylase 3
histone deacetylase 4
-
-
histone deacetylase 6
histone deacetylase 7
histone deacetylase 8
histone deacetylase-7
-
-
tubulin deacetylase
-
-
Zn(II)-dependent deacetylase
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
deacetylation
hydrolysis
deacetylation
SYSTEMATIC NAME
IUBMB Comments
histone amidohydrolase
A class of enzymes that remove acetyl groups from N6-acetyl-lysine residues on a histone. The reaction of this enzyme is opposite to that of EC 2.3.1.48, histone acetyltransferase. Histone deacetylases (HDACs) can be organized into three classes, HDAC1, HDAC2 and HDAC3, depending on sequence similarity and domain organization. Histone acetylation plays an important role in regulation of gene expression. In eukaryotes, HDACs play a key role in the regulation of transcription and cell proliferation [4]. May be identical to EC 3.5.1.17, acyl-lysine deacylase.
CAS REGISTRY NUMBER
COMMENTARY hide
9076-57-7
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
Reversibility
r=reversible
ir=irreversible
?=not specified
Ac-LGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
Boc-acetyl-Lys-7-amido-4-methylcoumarin + H2O
Boc-acetyl-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
Substrates: -
Products: -
?
Fluor de Lys HDAC substrate + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
AAKAVGK(Ac)VIPELN + H2O
AAKAVGKVIPELN + acetate
show the reaction diagram
Substrates: -
Products: -
?
Ac-DQK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-FEK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-GGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-GS(PO3)K(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-GSK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-IHK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-ILK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-KGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-KHK(acetyl)K(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
Ac-KSK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-KWK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-KYK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-LGK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
Ac-LIK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-LYK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-PFK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-VLK(acetyl)-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
acetyl-GAK(acetyl)-7-amido-4-methylcoumarin + H2O
acetyl-GAK-7-amino-4-methylcoumarin + acetate
show the reaction diagram
Substrates: -
Products: -
?
acetyl-tubulin + H2O
tubulin + acetate
show the reaction diagram
-
Substrates: major HDAC6 substrate
Products: -
?
acetylated histone + H2O
acetate + histone
show the reaction diagram
-
Substrates: -
Products: -
?
AFKFFQK(Ac)DRKMAL + H2O
AFKFFQKDRKMAL + acetate
show the reaction diagram
Substrates: -
Products: -
?
alpha-tubulin + H2O
?
show the reaction diagram
-
Substrates: splicing variant HDAC6p114 is intact in its deacetylase activity against a-tubulin
Products: -
?
alpha-tubulin + H2O
acetate + ?
show the reaction diagram
-
Substrates: -
Products: -
?
ASKRAFK(Ac)QSPPAV + H2O
ASKRAFKQSPPAV + acetate
show the reaction diagram
Substrates: -
Products: -
?
benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + acetate
show the reaction diagram
-
Substrates: -
Products: -
?
benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + trifluoroacetate
show the reaction diagram
-
Substrates: -
Products: -
?
Boc-Lys(ac)-coumarin + H2O
Boc-Lys-coumarin + acetate
show the reaction diagram
Substrates: i.e. Boc-K(ac)-Fluor-de-Lys
Products: -
?
Boc-trifluoroacetyl-Lys-7-amido-4-methylcoumarin + H2O
Boc-trifluoroacetyl-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
Substrates: -
Products: -
?
CKDLK(ac)RLFS + H2O
CKDLKRLFS + acetate
show the reaction diagram
Substrates: i.e. CREB94
Products: -
?
DPGNEVK(Ac)LKLYAL + H2O
DPGNEVKLKLYAL + acetate
show the reaction diagram
Substrates: -
Products: -
?
EANPGEK(Ac)RKMTDS + H2O
EANPGEKRKMTDS + acetate
show the reaction diagram
Substrates: -
Products: -
?
Fluor de Lys + H2O
?
show the reaction diagram
Fluor de Lys H4-AcK16 + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
Fluor de Lys HDAC substrate + H2O
?
show the reaction diagram
Fluor de Lys HDAC8 substrate + H2O
?
show the reaction diagram
GATYQDK(Ac)RYTNKY + H2O
GATYQDKRYTNKY + acetate
show the reaction diagram
Substrates: -
Products: -
?
GFGNGMK(Ac)QMRRTW + H2O
GFGNGMKQMRRTW + acetate
show the reaction diagram
Substrates: -
Products: -
?
GGK(Ac)FF + H2O
GGKFF + acetate
show the reaction diagram
Substrates: -
Products: -
?
GGMRGMK(Ac)GLVYET + H2O
GGMRGMKGLVYET + acetate
show the reaction diagram
Substrates: -
Products: -
?
GK(Ac)F + H2O
GKF + acetate
show the reaction diagram
Substrates: -
Products: -
?
HGGTILK(Ac)MIEEAG + H2O
HGGTILKMIEEAG + acetate
show the reaction diagram
Substrates: -
Products: -
?
LGDGK(ac)MKS + H2O
LGDGKMKS + acetate
show the reaction diagram
Substrates: i.e. THRAP3, low activity
Products: -
?
LGK(ac)FRR + H2O
LGKFRR + acetate
show the reaction diagram
Substrates: i.e. La-related protein 1, LARP1, best peptide substrate
Products: -
?
LYDRGTK(Ac)FGLFTP + H2O
LYDRGTKFGLFTP + acetate
show the reaction diagram
Substrates: -
Products: -
?
N-acetyl-arginine-histidine-acetyl-lysine-acetyl-lysine-coumarin + H2O
?
show the reaction diagram
Substrates: substrate in crystallized enzyme-substrate complex
Products: -
?
N-acetyl-lysine-alpha-tubulin + H2O
acetate + alpha-tubulin
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-heat shock protein 90 + H2O
acetate + heat shock protein 90
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-histone H3 + H2O
acetate + histone H3
show the reaction diagram
N-acetyl-lysine-histone H3 + H2O
histone H3 + acetate
show the reaction diagram
-
Substrates: deacetylation occurs at Lys9 and Lys23
Products: -
?
N-acetyl-lysine-histone H4 + H2O
acetate + histone H4
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-MyoD + H2O
acetate + MyoD
show the reaction diagram
N6-lysine acetylated histone H2A + H2O
histone H2A + acetate
show the reaction diagram
-
Substrates: substrate of isoforms HDAC1, HDAC2, HDAC. Isoform HDAC3 preferentially cleeaves lysines 5 H2A
Products: -
?
N6-lysine acetylated histone H3 + H2O
histone H3 + acetate
show the reaction diagram
N6-lysine acetylated histone H4 + H2O
histone H4 + acetate
show the reaction diagram
N6-lysine acetylated histone H4 peptide + H2O
histone H4 peptide + acetate
show the reaction diagram
Substrates: peptide of N-terminal 20 amino acids
Products: -
?
N6-lysine-acetylated histone H4 peptide + H2O
acetate + histone H4 peptide
show the reaction diagram
Substrates: -
Products: -
?
NARRKPK(Ac)GSPRVP + H2O
NARRKPKGSPRVP + acetate
show the reaction diagram
Substrates: -
Products: -
?
QSVQPSK(Ac)FNSYGR + H2O
QSVQPSKFNSYGR + acetate
show the reaction diagram
Substrates: -
Products: -
?
QTSPNPK(Ac)YRGFFH + H2O
QTSPNPKYRGFFH + acetate
show the reaction diagram
Substrates: -
Products: -
?
RGGK(Ac)FFR + H2O
RGGKFFR + acetate
show the reaction diagram
Substrates: -
Products: -
?
RHK(ac)K(ac)-coumarin + H2O
RHKK-coumarin + 2 acetate
show the reaction diagram
Substrates: i.e. HDAC8 Fluor-de-Lys or HDAC8 p53 FdL, low activity
Products: -
?
RHK(acetyl)K(acetyl)-fluorophore + H2O
RHKK-fluorophore + acetate
show the reaction diagram
RHKK(ac)-coumarin + H2O
RHKK-coumarin + acetate
show the reaction diagram
Substrates: i.e. SIRT1 Fluor-de-Lys
Products: -
?
RIANRTK(Ac)NSLTLQ + H2O
RIANRTKNSLTLQ + acetate
show the reaction diagram
Substrates: -
Products: -
?
RINSGGK(Ac)LPNFGF + H2O
RINSGGKLPNFGF + acetate
show the reaction diagram
Substrates: -
Products: -
?
RSLKYGK(Ac)VSPSLV + H2O
RSLKYGKVSPSLV + acetate
show the reaction diagram
Substrates: -
Products: -
?
RTSGRDK(Ac)YGPPVR + H2O
RTSGRDKYGPPVR + acetate
show the reaction diagram
Substrates: -
Products: -
?
RTSLGPK(Ac)SMMKML + H2O
RTSLGPKSMMKML + acetate
show the reaction diagram
Substrates: -
Products: -
?
RVIGAKK(ac)DQ + H2O
RVIGAKKDQ + acetate
show the reaction diagram
Substrates: a SMC3 9mer
Products: -
?
RVIGAKK(ac)DQY + H2O
RVIGAKKDQY + acetate
show the reaction diagram
Substrates: a SMC3 10mer
Products: -
?
RYSSRRK(Ac)ARPYML + H2O
RYSSRRKARPYML + acetate
show the reaction diagram
Substrates: -
Products: -
?
SQSEEEK(Ac)FFRRFP + H2O
SQSEEEKFFRRFP + acetate
show the reaction diagram
Substrates: -
Products: -
?
SRGGK(Ac)FFRR + H2O
SRGGKFFRR + acetate
show the reaction diagram
Substrates: -
Products: -
?
STPRFGK(Ac)TFDAPP + H2O
STPRFGKTFDAPP + acetate
show the reaction diagram
Substrates: -
Products: -
?
STPVK(ac)FISR + H2O
STPVKFISR + acetate
show the reaction diagram
Substrates: i.e. CSRP2BP
Products: -
?
tert-butyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + acetate
show the reaction diagram
TGKYFDK(Ac)ASYRVY + H2O
TGKYFDKASYRVY + acetate
show the reaction diagram
Substrates: -
Products: -
?
TKQTARK(ac)STGGKA + H2O
TKQTARKSTGGKA + acetate
show the reaction diagram
Substrates: a H3K9 13mer
Products: -
?
TLKKTGK(Ac)TVSYLG + H2O
TLKKTGKTVSYLG + acetate
show the reaction diagram
Substrates: -
Products: -
?
TYSRGGK(Ac)FFRRFP + H2O
TYSRGGKFFRRFP + acetate
show the reaction diagram
Substrates: -
Products: -
?
TYSRGGK(Ac)KSEESE + H2O
TYSRGGKKSEESE + acetate
show the reaction diagram
Substrates: -
Products: -
?
VLRNGGK(Ac)NFPAIF + H2O
VLRNGGKNFPAIF + acetate
show the reaction diagram
Substrates: -
Products: -
?
VRGFGGK(Ac)FGVQMD + H2O
VRGFGGKFGVQMD + acetate
show the reaction diagram
Substrates: -
Products: -
?
WEALGGK(Ac)AAYRTS + H2O
WEALGGKAAYRTS + acetate
show the reaction diagram
Substrates: -
Products: -
?
YSRGGK(Ac)FFRRF + H2O
YSRGGKFFRRF + acetate
show the reaction diagram
Substrates: -
Products: -
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
alpha-tubulin + H2O
?
show the reaction diagram
-
Substrates: splicing variant HDAC6p114 is intact in its deacetylase activity against a-tubulin
Products: -
?
alpha-tubulin + H2O
acetate + ?
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-alpha-tubulin + H2O
acetate + alpha-tubulin
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-heat shock protein 90 + H2O
acetate + heat shock protein 90
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-histone H3 + H2O
acetate + histone H3
show the reaction diagram
-
Substrates: -
Products: -
?
N-acetyl-lysine-MyoD + H2O
acetate + MyoD
show the reaction diagram
-
Substrates: transcription factor MyoD, its activity is co-dependent on isoform HDAC1 and transcriptional co-activator P/CAF
Products: -
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ATP
-
required for deacetylation of histone H4 in purified nucleosomes by isoforms HDAC1 and HDAC3. ATP also enhances cleavage of free, non-nucleosomal histones by HDAC1 and HDAC3
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Na+
-
Na+ binds more weakly to both monovalent cation sites and activates HDAC8 to a lesser extent than K+
Ni2+
ratio of kcat to KM value in presence of metal ion in decreasing order: Co(II), Fe(II), Zn(II), Ni(II)
additional information
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R,5S)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-6-oxabicyclo[3.1.1]heptane-3-carboxamide
(2E)-N-(2-aminophenyl)-3-(4-{1-[(2-hydroxyethyl)amino]-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl}phenyl)prop-2-enamide
-
(2E)-N-(2-aminophenyl)-3-(4-{1-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl}phenyl)prop-2-enamide
-
(2E)-N-(2-aminophenyl)-3-[4-(1-{[2-(morpholin-4-yl)ethyl]amino}-2-oxo-2-[4-(trifluoromethyl)anilino]ethyl)phenyl]prop-2-enamide
-
(2E)-N-(2-aminophenyl)-3-{4-[2-(4-bromoanilino)-1-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]phenyl}prop-2-enamide
-
(2R)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-2-carboxamide
-
(2S)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-2-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]-2-fluorophenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-benzyl-N-(4-chlorophenyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(3-methylphenyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(4-methylphenyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(6-methylpyridin-3-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(piperidin-1-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(propan-2-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-2-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-3-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-(pyridin-4-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-phenylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-[4-(propan-2-yl)phenyl]pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-1-methyl-N-[4-(trifluoromethyl)phenyl]pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2,4-difluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2-chloro-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(2-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3,4-dichlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3,4-difluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-bromo-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-chloro-4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(3-methoxyphenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-bromophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chloro-3-methylphenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2,2-trifluoroethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2-difluoroethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2,2-dimethylpropyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-fluoroethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(2-methoxyethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(3-hydroxy-2,2-dimethylpropyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(cyanomethyl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(propan-2-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-(pyrimidin-2-yl)pyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-cyclobutylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-ethylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-cyanophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-cyclopropylphenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-fluoro-3-methylphenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-fluorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-methoxyphenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(5-chloropyridin-2-yl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-cyclopentyl-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-cyclopropyl-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N~3~-(4-chlorophenyl)-N~1~,N~1~-diethylpyrrolidine-1,3-dicarboxamide
-
(3R)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N~3~-(4-chlorophenyl)-N~1~-ethylpyrrolidine-1,3-dicarboxamide
-
(3R)-4-{5-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyrazin-2-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{5-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridin-2-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{6-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridazin-3-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R)-4-{6-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]pyridin-3-yl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3R,4S)-4-{4-[(1E)-3-(2-aminoanilino)-3-oxoprop-1-en-1-yl]phenyl}-N-(4-chlorophenyl)-1-methylpyrrolidine-3-carboxamide
-
(3S,15R,20aS)-15-methyl-3-[(1E)-4-sulfanylbut-1-en-1-yl]-3,4,6,7,14,15,18,19,20,20a-decahydro-1H,5H,16H-11,8:15,12-di(azeno)pyrrolo[2,1-c][1,8,12,4,15]oxadithiadiazacyclooctadecine-1,5,16-trione
-
(4E)-N-(2-aminophenyl)-5-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]pent-4-enamide
-
(4Z)-6-[(5R,8S,11R)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-4-enoic acid
-
(5E)-N-(2-aminophenyl)-6-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-5-enamide
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3-thia-7,14,20,21-tetraazatricyclo[14.3.1.1-2,5]henicosa-1(20),2(21),16,18-tetraene-6,9,13-trione
-
(5R,8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8R,11R)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8S,11S,5'S,8'S,11'S)-11,11'-[disulfanediyldi(1E)but-1-ene-4,1-diyl]bis[5-methyl-8-(1-methylethyl)-3,10,17-trioxa-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione]
-
(8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),4,16(19)-tetraene-6,9,13-trione
-
(E)-3-(2-(((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)pyrimidin-5-yl)-N-hydroxyacrylamide
65% inhibition at 100 nM
(E)-N-hydroxy-3-(2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidin-5-yl)acrylamide
61% inhibition at 100 nM
(S)-N1-((S)-1-((2,4-difluorobenzyl)amino)-1-oxopropan-2-yl)-2-(4-((E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl)benzamido)-N4-neopentylsuccinamide
dual HDAC1/6 and proteasome inhibitor, selectivity HDAC1/HDAC6 is 0.27
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenylamide
-
2-(((3-(1-(2,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
88% inhibition at 100 nM
2-(((3-(1-(2-chloro-4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
73% inhibition at 100 nM
2-(((3-(1-(2-chlorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
93% inhibition at 100 nM
2-(((3-(1-(2-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
84% inhibition at 100 nM
2-(((3-(1-(4-cyanobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
68% inhibition at 100 nM
2-(((3-(1-(4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
92% inhibition at 100 nM
2-(((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
96% inhibition at 100 nM
2-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacetamide
18% inhibition at 100 nM
3-(4-((3-(1-(2,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
35% inhibition at 100 nM
3-(4-((3-(1-(2-chlorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
8% inhibition at 100 nM
3-(4-((3-(1-(2-cyanobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
36% inhibition at 100 nM
3-(4-((3-(1-(2-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
31% inhibition at 100 nM
3-(4-((3-(1-(3,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
17% inhibition at 100 nM
3-(4-((3-(1-(3-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
35% inhibition at 100 nM
3-(4-((3-(1-(4-bromobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
6% inhibition at 100 nM
3-(4-((3-(1-(4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
38% inhibition at 100 nM
3-(4-((3-(1-allylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
34% inhibition at 100 nM
3-(4-((3-(1-allylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxypropanamide
4% inhibition at 100 nM
3-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N- hydroxypropanamide
11% inhibition at 100 nM
3-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
35% inhibition at 100 nM
4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)-N-hydroxybenzamide
29% inhibition at 100 nM
5-(4-((1H-indol-3-yl)methyl)piperazin-1-yl)-N-(2-aminophenyl)pyrazine-2-carboxamide
inhibitor blocks HDAC1, HDAC2, and HDAC3
belinostat
i.e. PXD-101
chidamide
entinostat
-
HDAC1 siRNA
-
-
MC1568
specificity for class II HDACs
MC1575
specificity for class II HDACs
MCP30
30 kDa protein isolated from bitter melon seeds, Momordica charantia, contains two highly related type I ribosome-inactivating proteins, alpha- and beta-momorcharin
-
mocetinostat
-
MS-275
N-(2-amino-5-(thiophen-2-yl)phenyl)-5-(4-(2-(1-methyl-1H-indol-3-yl)ethyl)piperazin-1-yl)pyrazine-2-carboxamide
selective HDAC1/HDAC2 inhibitor
N-(2-amino-5-(thiophen-2-yl)phenyl)-5-(piperazin-1-yl)pyrazine-2-carboxamide
selective HDAC1/HDAC2 inhibitor
N-(2-amino-5-(thiophen-3-yl)phenyl)-5-(4-methylpiperazin-1-yl)pyrazine-2-carboxamide
highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes
N-(2-aminophenyl)-5-(4-((1-methyl-1H-indol-3-yl)methyl)piperazin-1-yl)pyrazine-2-carboxamide
highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes
N-(4-amino-3'-fluoro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-(4-amino-4'-chloro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3,4-dihydro-1H-2-benzopyran-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3,4-dihydro-2H-1-benzopyran-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3-oxabicyclo[3.1.0]hexane-6-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
i.e. BRD4884, possesses kinetic selectivity for isozyme HDAC1 versus HDAC2, inhibition kinetics
N-(4-amino[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-hydroxy-2-(methyl((3-(1-(3-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
93% inhibition at 100 nM
N-hydroxy-2-(methyl((3-(1-(4-(trifluoromethyl)benzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
62% inhibition at 100 nM
N-hydroxy-2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
96% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(2-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
14% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(2-nitrobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
19% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(3-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
25% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methoxybenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
36% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
32% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)propanamide
12% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-propylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
40% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-propylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)propanamide
5% inhibition at 100 nM
N-hydroxy-4-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}butanamide
-
N-hydroxy-5-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}pentanamide
-
N-hydroxy-6-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}hexanamide
-
N-hydroxy-7-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}heptanamide
-
N-hydroxy-8-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}octanamide
-
N-hydroxy-N~3~-[5-(propan-2-yl)naphthalene-1-sulfonyl]-beta-alaninamide
-
N-[(2E)-3-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]prop-2-en-1-yl]-2-sulfanylacetamide
-
N-[(3E)-4-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl]-2-sulfanylacetamide
-
N-[2-amino-5-(pyridin-3-yl)phenyl]oxane-4-carboxamide
-
N-[2-amino-5-(pyridin-4-yl)phenyl]oxane-4-carboxamide
-
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-(phenylsulfinylmethyl)-1H-1,2,3-triazol-4-yl]benzamide
single-step slow-binding mechanism
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-(phenylsulfonylmethyl)-1H-1,2,3-triazol-4-yl]benzamide
HDAC1/2-selective inhibitor, inhibits HDAC2 through a two-step slow-binding mechanism. In cellular assays, KPZ560 induces a dose- and time-dependent increase of histone acetylation and shows potent breast cancer cell growth-inhibitory activity
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-[2-(pyridin-2-yl)ethyl]-1H-1,2,3-triazol-4-yl]benzamide
single-step slow-binding mechanism
N-[4-amino-4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]oxane-4-carboxamide
-
panobinostat
resminostat
-
romidepsin
i.e. FK-228
SAHA
i.e. vorinostat
suberoylanilide hydroxamic acid
suberoylanilide trifluoromethylketone
-
trichostatin A
vorinostat
-
(1R,5S)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-6-oxabicyclo[3.1.1]heptane-3-carboxamide
(2E)-3-[1,2-bis(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-benzyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-benzyl-2-(2-phenylethyl)-1H-benzimidazol-6-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-ethyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[2-(diethylamino)ethyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[3-(dimethylamino)-2,2-dimethylpropyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[3-(dimethylamino)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[1-[4-(dimethylamino)butyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[2-cyclohexyl-1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[2-[(benzyloxy)methyl]-1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]-N-hydroxyprop-2-enamide
-
-
(2E)-3-[4-([[2-(3a,7a-dihydro-1H-indol-3-yl)ethyl](2-hydroxyethyl)amino]methyl)phenyl]-N-hydroxyprop-2-enamide
-
(2E)-N-(2-aminophenyl)-3-[2-(2-phenylethyl)-1-(pyridin-2-ylmethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-naphthalen-1-ylprop-2-enamide
-
HDAC8-selective inhibitor
(2E)-N-hydroxy-3-[1-(2-morpholin-4-ylethyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(1-methylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-methylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-phenylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-octyl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-hydroxypropyl)-2-thiophen-3-yl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-methoxypropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-(3-morpholin-4-ylpropyl)-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-methyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-[3-(1H-imidazol-1-yl)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[1-[3-(2-oxopyrrolidin-1-yl)propyl]-2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(2-piperidin-1-ylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(2-pyrrolidin-1-ylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(3,4,5-trimethoxybenzyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(3-pyrrolidin-1-ylpropyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-(pyridin-2-ylmethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1-propyl-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-(2-phenylethyl)-1H-benzimidazol-5-yl]prop-2-enamide
-
-
(2E)-N-hydroxy-3-[2-[(4-methoxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.93 microM
(2E)-N-hydroxy-3-[2-[2-(1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.22 microM
(2E)-N-hydroxy-3-[2-[2-(2-methyl-1H-indol-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.1042microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation
(2E)-N-hydroxy-3-[2-[2-(pyrazolo[1,5-a]pyridin-3-yl)ethyl]-2,3-dihydro-1H-isoindol-5-yl]prop-2-enamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.53 microM. Compound has a reasonable combination of potency, solubility and human microsomal stability to justify further investigation
(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
-
(2R)-methyl-1-[4-[4-(2-aminoacetamido)phenyl]benzenesulfonyl]pyrrolidine-2-carboxylate
activities against Hela cells with IC50 0.31 microM, not cytotoxic to normal cells. The alpha-amino amide moiety of the compound coordinates with the zinc ion of HDAC6 in a bidentate chelate manner
(2R)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-2-carboxamide
-
(2S)-2-(acetylamino)-3-[3-[(2S)-2-[[(2S)-2-ammonio-7-(hydroxyamino)-7-oxoheptanoyl]amino]-3-methoxy-3-oxopropyl]phenyl]propanoate
-
-
(2S)-8-oxo-2-[(3-piperidin-1-ylpropanoyl)amino]-N-quinolin-3-ylnonanamide
-
-
(2S)-N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-2-carboxamide
-
(3S)-3-{[(3S)-3-{[(benzyloxy)carbonyl]amino}-3-cyclopropylpropanoyl]amino}-2-oxo-5-phenylpentyl acetate
-
-
(3S,15R,20aS)-15-methyl-3-[(1E)-4-sulfanylbut-1-en-1-yl]-3,4,6,7,14,15,18,19,20,20a-decahydro-1H,5H,16H-11,8:15,12-di(azeno)pyrrolo[2,1-c][1,8,12,4,15]oxadithiadiazacyclooctadecine-1,5,16-trione
-
(3S,6S,10S,14S)-3-(1H-indol-3-ylmethyl)-10-methyl-14-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,11-tetraazacyclotetradecane-2,5,8,12-tetrone
-
-
(3S,6S,9S,13S)-3-(1H-indol-3-ylmethyl)-9,10-dimethyl-13-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
-
(3S,6S,9S,13S)-3-(1H-indol-3-ylmethyl)-9-methyl-13-(2-methylpropyl)-6-(6-oxooctyl)-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
-
(3S,6S,9S,15aS)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-3-(6-oxooctyl)decahydro-1H-pyrrolo[1,2-a][1,4,7,10]tetraazacyclotridecine-1,4,7,11(8H)-tetrone
-
-
(4E)-N-(2-aminophenyl)-5-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]pent-4-enamide
-
(4Z)-6-[(5R,8S,11R)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-4-enoic acid
-
(5E)-N-(2-aminophenyl)-6-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]hex-5-enamide
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5R,8S,11S)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3-thia-7,14,20,21-tetraazatricyclo[14.3.1.1-2,5]henicosa-1(20),2(21),16,18-tetraene-6,9,13-trione
-
(5R,8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8R,11R)-5-methyl-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione
-
(5S,8S,11S,5'S,8'S,11'S)-11,11'-[disulfanediyldi(1E)but-1-ene-4,1-diyl]bis[5-methyl-8-(1-methylethyl)-3,10,17-trioxa-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione]
-
(8S,11S)-8-(1-methylethyl)-11-[(1E)-4-sulfanylbut-1-en-1-yl]-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),4,16(19)-tetraene-6,9,13-trione
-
(E)-3-(2-(((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)pyrimidin-5-yl)-N-hydroxyacrylamide
55% inhibition at 100 nM
(E)-3-[3-[4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl]phenyl]-N-hydroxyacrylamide
-
inhibitor for both EGFR/HER2 kinase and HDAC with potent cellular activity, i.e. target inhibition and cytotoxicity
(E)-N-hydroxy-3-(2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidin-5-yl)acrylamide
60% inhibition at 100 nM
(E)-N1-hydroxy-N5-(5-styryl-1,3,4-thiadiazol-2-yl)glutaramide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0059 and 0.00675 microM, respectively
(S)-5-cyclopropyl-N-(1-(4-(hydroxycarbamoyl)phenyl)-ethyl)-5'-phenyl-[2,2'-bithiazole]-4-carboxamide
compound displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound has a favorable pharmacokinetic profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-(naphthalen-1-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-m-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-o-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-p-tolyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-pentyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-phenethyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-7-(2-(hydroxyamino)-2-oxoethoxy)-N-phenyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride
-
(S)-benzyl 3-(biphenyl-4-ylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-benzyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenethylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-benzyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-N-(2,4-dimethylphenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-(3-chloro-4-fluorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-(3-chlorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-(4-fluorophenyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-(biphenyl-4-yl)-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-benzyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride
-
(S)-N-hexyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-N-tert -butyl-7-(2-(hydroxyamino)-2-oxoethoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
(S)-tert-butyl 3-(2,4-dimethylphenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(3-chloro-4-fluorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(3-chlorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(4-fluorophenylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(benzylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(biphenyl-4-ylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(hexylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 3-(tert-butylcarbamoyl)-7-(2-(hydroxyamino)-2-oxoethoxy)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(4-methoxyphenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(mtolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(naphthalen-1-ylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(o-tolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(p-tolylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(pentylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenethylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
(S)-tert-butyl 7-(2-(hydroxyamino)-2-oxoethoxy)-3-(phenylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
-
1-methyl-N-[(1S)-7-oxo-1-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]octyl]piperidine-2-carboxamide
-
-
1-[5-(2,3-dihydro-1,4-benzodioxin-6-yl)thiophen-2-yl]-2,2,2-trifluoroethanone
-
-
1-[5-(4-acetylphenyl)thiophen-2-yl]-2,2,2-trifluoroethanone
-
-
15-deoxy-DELTA12,14-prostaglandin J2-biotin
-
maximal inhibition of recombinant HDAC3 in complex with CoR1 is 50%
2,2,2-trifluoro-1-(2-phenyl-1,3-thiazol-5-yl)ethanone
-
-
2,2,2-trifluoro-1-(4-phenylthiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-phenylthiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-[3-[(methylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
potent inhibitor of HDAC4 and shows more than 100fold selectivity overHDAC1
2,2,2-trifluoro-1-(5-[3-[(propylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-(5-[3-[(thiophen-2-ylsulfonyl)methyl]-1,2,4-oxadiazol-5-yl]thiophen-2-yl)ethanone
-
-
2,2,2-trifluoro-1-[5-(1H-indol-5-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(2-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(3-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(3-methyl-1,2,4-oxadiazol-5-yl)thiophen-2-yl]ethanone
-
HDAC4-selective inhibitor
2,2,2-trifluoro-1-[5-(3-[[(4-fluorobenzyl)sulfonyl]methyl]-1,2,4-oxadiazol-5-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(4-methoxyphenyl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(pyridin-2-yl)thiophen-2-yl]ethanone
-
-
2,2,2-trifluoro-1-[5-(quinoxalin-6-yl)thiophen-2-yl]ethanone
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide
-
-
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide
-
competitive. Significant but rather unselective inhibition of cellular HDACs
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenylamide
-
2,3-dihydrobenzoic acid
98% residual activity at 0.5 mM
2-(((3-(1-(2,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
66% inhibition at 100 nM
2-(((3-(1-(2-chloro-4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
49% inhibition at 100 nM
2-(((3-(1-(2-chlorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
55% inhibition at 100 nM
2-(((3-(1-(2-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
44% inhibition at 100 nM
2-(((3-(1-(4-cyanobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
38% inhibition at 100 nM
2-(((3-(1-(4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
65% inhibition at 100 nM
2-(((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)(methyl)amino)-N-hydroxypyrimidine-5-carboxamide
63% inhibition at 100 nM
2-(3,6-dihydroxy-9H-xanthen-9-yl)-5-(8-(hydroxyamino)-8-oxooctanamido)benzoic acid
synthesis, overview
2-(3,6-dihydroxy-9H-xanthen-9-yl)-5-(8-methoxy-8-oxooctanamido)benzoic acid
synthesis, overview
2-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacetamide
35% inhibition at 100 nM
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
-
-
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
-
-
2-hydroxybutyric acid
96% residual activity at 0.5 mM
2-[(methylsulfonyl)sulfanyl]ethanaminium bromide
-
-
2-[(methylsulfonyl)sulfanyl]ethyl 2-propylpentanoate
-
-
3,4-Dihydroxyphenyl acetic acid
90% residual activity at 0.5 mM
3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide
APHA
3-(4-((3-(1-(2,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
74% inhibition at 100 nM
3-(4-((3-(1-(2-chlorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
59% inhibition at 100 nM
3-(4-((3-(1-(2-cyanobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
65% inhibition at 100 nM
3-(4-((3-(1-(2-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
68% inhibition at 100 nM
3-(4-((3-(1-(3,4-difluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
60% inhibition at 100 nM
3-(4-((3-(1-(3-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
73% inhibition at 100 nM
3-(4-((3-(1-(4-bromobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
58% inhibition at 100 nM
3-(4-((3-(1-(4-fluorobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
75% inhibition at 100 nM
3-(4-((3-(1-allylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
66% inhibition at 100 nM
3-(4-((3-(1-allylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxypropanamide
15% inhibition at 100 nM
3-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N- hydroxypropanamide
22% inhibition at 100 nM
3-(4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)-N-hydroxyacrylamide
71% inhibition at 100 nM
3-hydroxycinnamic acid
96% residual activity at 0.5 mM
3-[5-(trifluoroacetyl)thiophen-2-yl]benzoic acid
-
the inhibitor shows 40fold selectivity for HDAC4 and 180fold for HDAC6 against HDAC1
3-[5-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]-2-(2-phenylethyl)-1H-benzimidazol-1-yl]propanoic acid
-
-
3-[5-[4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl]furan-2-yl]-N-hydroxy-acrylamide
-
inhibitor for both EGFR/HER2 kinase and HDAC with potent cellular activity, i.e. target inhibition and cytotoxicity
4-((3-(1-benzylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)-N-hydroxybenzamide
66% inhibition at 100 nM
4-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl 2-propylpentanoate
-
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
M344
4-hydroxy-2-nonenal
-
maximal inhibition of recombinant HDAC3 in complex with CoR1 is 70%
4-[5-(trifluoroacetyl)thiophen-2-yl]benzoic acid
-
-
4-[5-(trifluoroacetyl)thiophen-2-yl]benzonitrile
-
-
4-[[(2E)-2-(2-chlorobenzylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
-
4-[[(2E)-2-(4-chlorobenzylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
inactivates HDAC8 preferentially over HDAC1
4-[[(2E)-2-(anthracen-9-ylmethylidene)hydrazinyl]carbonothioyl]-N-hydroxypiperazine-1-carboxamide
-
4-[[2-(3-chlorophenyl)-1'-methylspiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-N-hydroxybenzamide
spiroindoline derivative, binding next to Trp198, on the enzyme surface
4-[[2-(4-chlorophenyl)-1'-methylspiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-N-hydroxybenzamide
spiroindoline derivative, binding next to Trp198, on the enzyme surface
5-((2-(3-chlorophenyl)-1'-methylspiro[indoline-3,4'-piperidin]-1-yl)methyl)-N-hydroxythiophene-2-carboxamide
spiroindoline derivative, binding next to Trp198, on the enzyme surface
5-((2-(4-chlorophenyl)-1'-methylspiro[indoline-3,4'-piperidin]-1-yl)methyl)-N-hydroxythiophene-2-carboxamide
spiroindoline derivative, binding next to Trp198, on the enzyme surface
5-(4-((1H-indol-3-yl)methyl)piperazin-1-yl)-N-(2-aminophenyl)pyrazine-2-carboxamide
inhibitor blocks HDAC1, HDAC2, and HDAC3
5-(4-benzyl-1H-1,2,3-triazol-1-yl)-N-hydroxypentanamide
-
-
5-(4-hydroxyphenyl)-3H-1,2-dithiol-3-thione
-
-
5-[(7-bromo-2-phenyl-2,3-dihydro-4H-thieno[3,2-b]indol-4-yl)methyl]-N-hydroxythiophene-2-carboxamide
-
5-[(7-fluoro-2-phenyl-2,3-dihydro-4H-thieno[3,2-b]indol-4-yl)methyl]-N-hydroxythiophene-2-carboxamide
-
6-mercapto-N-phenylhexanamide
-
6-[(1-(mercaptomethyl)vinyl)amino]-N-phenylhexanamide
-
6-[(2S,5S,8S,11S)-8-(1H-indol-3-ylmethyl)-2-methyl-11-(2-methylpropyl)-3,6,9,13-tetraoxo-1,4,7,10-tetraazacyclotridecan-5-yl]hexanoic acid
-
-
6-[(9H-fluoren-3-ylmethyl)(3-phenoxybenzyl)amino]-N-hydroxyhexanamide
-
-
6-[(biphenyl-4-ylmethyl)[4-[(4-bromobenzyl)oxy]benzyl]amino]-N-hydroxyhexanamide
-
-
6-[4-(2,6-dimethoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-2-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-3-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyhexanamide
-
-
6-[[4-[(4-bromobenzyl)oxy]benzyl](9H-fluoren-3-ylmethyl)amino]-N-hydroxyhexanamide
-
-
6-{4-[4-(dimethylamino)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyhexanamide
-
-
7-mercapto-N-(2-phenyl-1,3-thiazol-5-yl)heptanamide
-
7-mercapto-N-(3-phenoxyphenyl)heptanamide
-
7-mercapto-N-phenylheptanamide
thiol formed by enzymatic hydrolysis in the cell reacts with the zinc ion in the active site of histone deacetylase. Molecular modeling of complex with histone HDAC8
7-mercapto-N-pyridin-3-ylheptanamide
-
7-mercapto-N-quinolin-3-ylheptanamide
-
7-[4-(biphenyl-3-yl)-1H-1,2,3-triazol-1-yl]-N-hydroxyheptanamide
-
-
7-{4-[4-(dimethylamino)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyheptanamide
-
-
8-hydroxyquinoline
85% residual activity at 0.5 mM
acetylated histone deacetylase 1
-
the activity of HDAC2 is inhibited by acetylated HDAC1
-
allyl mercaptan
garlic organosulfur compounds can be metabolized to allyl mercaptan
alpha-keto-gamma-methylselenobutyrate
causes dose-dependent inhibition of HDAC activity, HDAC1 shows about 80% residual activity at 2 mM, HDAC8 shows less than 60% residual activity at 2 mM
apicidin
apicidin A
-
-
azumamide A
-
-
azumamide E
-
-
Baclofen
98% residual activity at 0.5 mM
belinostat
beta-methylselenopyruvate
causes dose-dependent inhibition of HDAC activity, competitive inhibitor of HDAC8, HDAC1 shows about 30% residual activity at 2 mM, HDAC8 shows less than 30% residual activity at 2 mM
Butyrate
Butyric acid
caffeic acid
80% residual activity at 0.5 mM
chlorogenic acid
highly potent HDAC inhibitor, 40% residual activity at 0.5 mM
Cinnamic acid
95% residual activity at 0.5 mM
curcumin
highly potent HDAC inhibitor, 52% residual activity at 0.5 mM
D-(-)-quinic acid
96% residual activity at 0.5 mM
dihydrocaffeic acid
86% residual activity at 0.5 mM
entinostat
-
MS-275
ferulic acid
80% residual activity at 0.5 mM
FK-228
FK228
-
-
FOXP
-
FOXP3 specifically inhibits binding of histone deacetylase 2 and 4 to the site and increases local histone H3 acetylation
-
FR235222
-
-
FR901375
-
-
gamma-aminobutyric acid
-
HC-toxin
-
-
indol-2-carboxylic acid
97% residual activity at 0.5 mM
isobutyric acid
80% residual activity at 0.5 mM
Isothiocyanate
found in cruciferous vegetables
ITF-2357
JNJ-26481585
-
broad-spectrum or pan-HDAC inhibitor
K+
-
K+ bound to monovalent cation site 1 inhibits catalytic activity of HDAC8 (11fold less active with two K+ ions bound compared to one K+ ion bound), partial inhibition at high KCl
LAQ-824
-
-
LAQ824
largazole
LBH-589
LBH589
Mandelic acid
85% residual activity at 0.5 mM
MC1568
specificity for class II HDACs
MC1575
specificity for class II HDACs
MC1863
-
-
methyl (3R,6R,9R)-9-(acetylamino)-6-[6-(hydroxyamino)-6-oxohexyl]-5,8-dioxo-4,7-diazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3-carboxylate
-
tight binding competitive inhibition
methyl N-[(2S)-2-[(N-acetyl-L-alanyl)amino]-7-(hydroxyamino)-7-oxoheptanoyl]-L-phenylalaninate
-
-
MGCD-0103
MS-275
N-(2,2-dimethylpropyl)-N2-[4-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]benzoyl]-L-asparaginyl-N-[(2,4-difluorophenyl)methyl]-L-alaninamide
dual HDAC1/6 and proteasome inhibitor, selectivity HDAC1/HDAC6 is 0.27
N-(2-amino-5-(thiophen-2-yl)phenyl)-5-(4-(2-(1-methyl-1H-indol-3-yl)ethyl)piperazin-1-yl)pyrazine-2-carboxamide
selective HDAC1/HDAC2 inhibitor
N-(2-amino-5-(thiophen-2-yl)phenyl)-5-(piperazin-1-yl)pyrazine-2-carboxamide
selective HDAC1/HDAC2 inhibitor
N-(2-amino-5-(thiophen-3-yl)phenyl)-5-(4-methylpiperazin-1-yl)pyrazine-2-carboxamide
highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes
N-(2-aminophenyl)-4-[[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]methyl]benzamide
-
-
N-(2-aminophenyl)-4-[[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]methyl]benzamide
-
-
N-(2-aminophenyl)-5-(4-((1-methyl-1H-indol-3-yl)methyl)piperazin-1-yl)pyrazine-2-carboxamide
highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes
N-(2-aminophenyl)-5-[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-aminophenyl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-aminophenyl)-6-(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(2-aminophenyl)-6-(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(2-aminopyridin-3-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(2-hydroxyphenyl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(4-amino-3'-fluoro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-(4-amino-4'-chloro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3,4-dihydro-1H-2-benzopyran-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3,4-dihydro-2H-1-benzopyran-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)-3-oxabicyclo[3.1.0]hexane-6-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-3-carboxamide
-
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
N-(4-aminopyrimidin-5-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(4-amino[1,1'-biphenyl]-3-yl)oxane-4-carboxamide
-
N-(6-mercaptohexyl)-1-benzofuran-2-carboxamide
-
N-(6-mercaptohexyl)-1H-indole-2-carboxamide
-
N-(6-mercaptohexyl)-2-naphthamide
-
N-(6-mercaptohexyl)benzamide
-
N-(8-aminonaphthalen-1-yl)-5-[(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(8-aminonaphthalen-1-yl)-5-[(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)sulfanyl]pentanamide
-
-
N-(8-aminonaphthalen-1-yl)-6-(4-biphenyl-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-(8-aminonaphthalen-1-yl)-6-(6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)hexanamide
-
-
N-biphenyl-3-yl-7-mercaptoheptanamide
-
N-hydroxy-1-(3-hydroxypropyl)-2-(2-phenylethyl)-1H-benzimidazole-5-carboxamide
-
-
N-hydroxy-1-methyl-indole-6-carboxamide
-
HDAC8-selective inhibitor
N-hydroxy-2-(methyl((3-(1-(3-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
54% inhibition at 100 nM
N-hydroxy-2-(methyl((3-(1-(4-(trifluoromethyl)benzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
30% inhibition at 100 nM
N-hydroxy-2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide
71% inhibition at 100 nM
N-hydroxy-2-[1-methyl-2-(2-phenylethyl)-1H-benzimidazol-5-yl]cyclopropanecarboxamide
-
-
N-hydroxy-3-(4-((3-(1-(2-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
68% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(2-nitrobenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
63% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(3-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
73% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methoxybenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
75% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
76% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)propanamide
28% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-propylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)acrylamide
69% inhibition at 100 nM
N-hydroxy-3-(4-((3-(1-propylpiperidin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)phenyl)propanamide
13% inhibition at 100 nM
N-hydroxy-3-[1-(3-hydroxypropyl)-2-(2-methylpropyl)-1H-benzimidazol-5-yl]propanamide
-
-
N-hydroxy-3-[2-(2-phenylethyl)-1-(3,4,5-trimethoxybenzyl)-1H-benzimidazol-5-yl]propanamide
-
-
N-hydroxy-3-[2-[(2-methyl-1H-indol-3-yl)acetyl]-2,3-dihydro-1H-isoindol-5-yl]propanamide
-
anti-proliferative activity in human HCT116 cell line, IC50 0.19 microM
N-hydroxy-4-(methyl[(5-pyridin-2-yl-2-thienyl)sulfonyl]amino)benzamide
-
N-hydroxy-4-[[(2E)-2-(2-hydroxybenzylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
inactivates HDAC8 preferentially over HDAC1
N-hydroxy-4-[[(2E)-2-(4-methylbenzylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
-
N-hydroxy-4-[[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazinyl]carbonothioyl]piperazine-1-carboxamide
-
N-hydroxy-4-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}butanamide
-
N-hydroxy-5-(4-phenyl-1H-1,2,3-triazol-1-yl)pentanamide
-
-
N-hydroxy-5-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}pentanamide
-
N-hydroxy-6-(4-phenyl-1H-1,2,3-triazol-1-yl)hexanamide
-
-
N-hydroxy-6-[(2S,5S,8S,11S)-8-(1H-indol-3-ylmethyl)-2-methyl-11-(2-methylpropyl)-3,6,9,13-tetraoxo-1,4,7,10-tetraazacyclotridecan-5-yl]hexanamide
-
-
N-hydroxy-6-[(3S,6S,9S,15aS)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-1,4,7,11-tetraoxotetradecahydro-1H-pyrrolo[1,2-a][1,4,7,10]tetraazacyclotridecin-3-yl]hexanamide
-
-
N-hydroxy-6-[4-(2-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(3-methylphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(4-methylphenyl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(6-methoxynaphthalen-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(pyridin-4-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(quinolin-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(quinolin-7-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-[4-(thiophen-2-yl)-1H-1,2,3-triazol-1-yl]hexanamide
-
-
N-hydroxy-6-{4-[4-(pyridin-4-yl)phenyl]-1H-1,2,3-triazol-1-yl}hexanamide
-
-
N-hydroxy-6-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}hexanamide
-
N-hydroxy-7-(4-phenyl-1H-1,2,3-triazol-1-yl)heptanamide
-
-
N-hydroxy-7-[4-(6-methoxynaphthalen-2-yl)-1H-1,2,3-triazol-1-yl]heptanamide
-
-
N-hydroxy-7-[4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl]heptanamide
-
-
N-hydroxy-7-{4-[4-(pyridin-4-yl)phenyl]-1H-1,2,3-triazol-1-yl}heptanamide
-
-
N-hydroxy-7-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}heptanamide
-
N-hydroxy-8-{[5-(propan-2-yl)naphthalene-1-sulfonyl]amino}octanamide
-
N-hydroxy-N~3~-[5-(propan-2-yl)naphthalene-1-sulfonyl]-beta-alaninamide
-
N-hydroxynaphthalene-1-carboxamide
-
HDAC8-selective inhibitor
N-methyl-N-(quinoxalin-6-ylmethyl)-5-(trifluoroacetyl)thiophene-2-carboxamide
-
-
N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
-
-
N-[(2E)-3-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]prop-2-en-1-yl]-2-sulfanylacetamide
-
N-[(3E)-4-[(5R,8S,11S)-5-methyl-8-(1-methylethyl)-6,9,13-trioxo-10-oxa-3,17-dithia-7,14,19,20-tetraazatricyclo[14.2.1.1-2,5]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-en-1-yl]-2-sulfanylacetamide
-
N-[2-amino-5-(pyridin-3-yl)phenyl]oxane-4-carboxamide
-
N-[2-amino-5-(pyridin-4-yl)phenyl]oxane-4-carboxamide
-
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-(phenylsulfinylmethyl)-1H-1,2,3-triazol-4-yl]benzamide
single-step slow-binding mechanism
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-(phenylsulfonylmethyl)-1H-1,2,3-triazol-4-yl]benzamide
HDAC1/2-selective inhibitor, inhibits HDAC2 through a two-step slow-binding mechanism. In cellular assays, KPZ560 induces a dose- and time-dependent increase of histone acetylation and shows potent breast cancer cell growth-inhibitory activity
N-[2-amino-5-(thiophen-2-yl)phenyl]-4-[1-[2-(pyridin-2-yl)ethyl]-1H-1,2,3-triazol-4-yl]benzamide
single-step slow-binding mechanism
N-[4-amino-4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]oxane-4-carboxamide
-
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N7-hydroxyheptanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0061 and 0.0122 microM, respectively
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N8-hydroxyoctanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00298 and 0.0091 microM, respectively
N1-hydroxy-N7-(5-phenyl-1,3,4-thiadiazol-2-yl)heptanediamide
-
antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0055 and 0.0129 microM, respectively
N1-hydroxy-N8-(5-phenyl-1,3,4-thiadiazol-2-yl)octanediamide
-
-
N1-methyl-2-oxo-N9-phenylnonanediamide
-
NVP-LAQ824
-
oxamflatin
-
p300
-
p300 can inactivate HDAC6 by acetylation
-
panobinostat
PAOA
-
-
PCI-24781
-
broad-spectrum or pan-HDAC inhibitor
PCI-34051
-
HDAC8-selective inhibitor
peroxynitrite
activity of wild-type enzyme is reduced to 38% in presence of peroxynitrite. Activities of mutants Y153A and Y253A are 233 completely abolished in the presence of peroxynitrite. Mutant Y146A shows 32% reduction in activity
phenyl butyric acid
-
phenylbutyrate
Buphenyl
phenylbutyric acid
-
propionic acid
80% residual activity at 0.5 mM
PXD-101
PXD101
-
-
pyridin-3-ylmethyl (4-[[(2-aminophenyl)amino]carbonyl]benzyl)carbamate
i.e. MS27-275
romidepsin
S-(2-hydroxyethyl) methanesulfonothioate
-
-
S-nitrosocysteine
the activity of HDAC8 is significantly inhibited when incubated with S-nitrosoglutathione and S-nitrosocysteine in a time- and dosage-dependent manner. Sodium nitroprusside and dithiothreitol cannot reverse this inhibition
S-nitrosoglutathione
HDAC8 can be S-nitrosylated by S-nitrosoglutathione in vitro, and the activity of HDAC8 is significantly inhibited when incubated with S-nitrosoglutathione and S-nitrosocysteine in a time- and dosage-dependent manner. Sodium nitroprusside and dithiothreitol cannot reverse this inhibition
S-[2-[(2-propylpentanoyl)amino]ethyl]methanesulfonothioate
-
-
S-[7-oxo-7-(2-phenyl1,3-thiazol-5-ylamino)heptyl] 2-methylpropanethioate
analysis of growth inhibition of various cancer cells and comparison with suberoylanilide hydroxamic acid
salicylic acid
92% residual activity at 0.5 mM
scriptaid
-
-
shRNA
-
-
-
SK7041
-
i.e. 4-dimethylamino-N-[4-(2-hydroxylcarbamoyl-vinyl)benzyl] benzamide
sodium butyrate
sodium phenylbutyrate
-
sorbic acid
91% residual activity at 0.5 mM
spiruchostatin
-
-
suberoyl anilide hydroxamic acid
suberoylanilide hydroxamic acid
suberoylanilide trifluoromethylketone
-
sulforaphane
tartaric acid
90% residual activity at 0.5 mM
trapoxin
trapoxin A
-
-
trapoxin B
trichostatin A
troglitazone
-
-
tubacin
Valeric acid
83% residual activity at 0.5 mM
Valproate
-
class I-selective HDAC inhibitor
Valproic acid
vorinostat
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
N-(cyclohexylcarbamothioyl)benzamide
-
10 microM, 5.6fold activation of HDAC8. No activation of other HDAC isoenzymes
N-(phenylcarbamothioyl)benzamide
-
10 microM, 12fold activation of HDAC8. No activation of other HDAC isoenzymes
N-[(3,5-dimethoxyphenyl)carbamothioyl]benzamide
-
10 microM, 8.4fold activation of HDAC8. No activation of other HDAC isoenzymes