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Information on EC 2.7.11.22 - cyclin-dependent kinase and Organism(s) Homo sapiens and UniProt Accession Q00532

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IUBMB Comments
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation.
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Homo sapiens
UNIPROT: Q00532
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Synonyms
cdk, p34cdc2, cdc2 kinase, cyclin-dependent kinase 5, cdc28, cyclin-dependent kinase 2, cyclin-dependent kinase 4, cyclin-dependent kinase 1, cdc42p, pho85, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cdc2
247
-
CDC2 kinase
247
-
CDC2deltaT
266073
a variant of human CDC2, that lacks 171 nucleotides corresponding to 57 amino acids, which compose most of the T-loop
Cdk 2
247
-
Cdk1/Cyclin B
247
-
Cdk1/cyclin B1 kinase
247
-
CDK10
247
-
CDK11
247
-
CDK11p110
266081
-
CDK12
266148
isoform
CDK13
306155
isoform
CDK3
247
-
CDK4 kinase
247
-
cdk5/p25 kinase
247
-
cell division control protein 2 homolog
266073
-
cell division cycle 2-related protein kinase 7
266148
-
cell division protein kinase 10
266141
-
cell division protein kinase 3
266120
-
cell division protein kinase 4
266075
-
cell division protein kinase 5
266123
-
cell division protein kinase 6
266122
-
cell division protein kinase 7
266113
-
cell division protein kinase 9
266114
-
cyclin A-cyclin-dependent kinase 2
247
-
cyclin A-dependent protein kinase 2
247
-
cyclin A/Cdk2
247
-
cyclin A2/Cdk2
247
-
cyclin dependent kinase 2
247
-
cyclin-dependent kinase
247
-
cyclin-dependent kinase 1
cyclin-dependent kinase 11p110
266081
-
cyclin-dependent kinase 11p58
247
-
cyclin-dependent kinase 2
cyclin-dependent kinase 4
247
-
cyclin-dependent kinase 5
cyclin-dependent kinase 6
247
-
cyclin-dependent kinase 7
266113
as part of the CDK-activating kinase complex, CDK7 is a component of the basal transcription factor TFIIH
cyclin-dependent kinase 8
266111
-
cyclin-dependent kinase 9
Cyclin-dependent kinase pef1
-
-
-
-
cyclin-dependent kinase-2
cyclin-dependent kinase-8
247
-
cyclin-dependent kinases 7
247
-
cyclin-dependent kinases 9
247
-
cyclin-dependent protein kinase 5
247
-
galactosyltransferase associated protein kinase p58/GTA
266081
-
K-cyclin/cdk6 kinase
247
-
K35
266111
-
kinase Cdk6
266122
-
male germ cell-associated kinase
266079
-
MO15/CDK7
266113
-
p25-Cdk5 kinase complex
247
-
p27 cyclin dependent kinase
247
-
p40MO15
266113
-
p58clk-1 protein kinase
266081
-
PFTK1
247
-
PFTK1/CCND3 complex
247
-
PHO85 homolog
-
-
-
-
PISSLRE
266141
-
PITALRE
266114
-
PITSLRE
266081
formerly
serine/threonine kinase p
266064
-
serine/threonine protein kinase PCTAIRE-3
266138
-
serine/threonine-protein kinase ALS2CR7
266147
-
serine/threonine-protein kinase KKIALRE
266121
-
serine/threonine-protein kinase MAK
266079
-
serine/threonine-protein kinase PCTAIRE-1
266124
-
serine/threonine-protein kinase PCTAIRE-2
266125
-
STK9
266064
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
catalytic aspartate residue
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:cyclin phosphotransferase
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation.
CAS REGISTRY NUMBER
COMMENTARY hide
150428-23-2
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
-
-
-
-
?
ATP + axonal cytoskeleton protein
ADP + phosphorylated axonal cytoskeleton protein
show the reaction diagram
ATP + biotin-TVSEESNVLCLSKSPNKHNRLYMKARPFF
ADP + biotin-TVSEESNVLCLSKpSPNKHNRLYMKARPFF
show the reaction diagram
-
-
phosphorylated on Ser595
-
?
ATP + bloom syndrome helicase
ADP + phosphorylated bloom syndrome helicase
show the reaction diagram
ATP + BRCA2
ADP + phosphorylated BRCA2
show the reaction diagram
ATP + c-Jun N-terminal kinase 3
ADP + phosphorylated c-Jun N-terminal kinase 3
show the reaction diagram
ATP + C-terminal domain of RNA polymerase II
ADP + phosphorylated C-terminal domain of RNA polymerase II
show the reaction diagram
ATP + CALD1 protein
ADP + CALD1 phosphoprotein
show the reaction diagram
-
reccombinant human GST-tagged substrate, with CDK6
-
-
?
ATP + Cdc20
ADP + phosphorylated Cdc20
show the reaction diagram
ATP + Cdc6
ADP + phosphorylated Cdc6
show the reaction diagram
-
-
-
-
?
ATP + CDK1
ADP + phosphorylated CDK1
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK1
-
-
?
ATP + Cdk1
ADP + phosphorylated Cdk2
show the reaction diagram
-
Cdk7
-
-
?
ATP + cdk2
ADP + phosphorylated cdk2
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK2
-
-
?
ATP + Cprk
ADP + phosphorylated Cprk
show the reaction diagram
-
i.e. Cdk5/p35-regulated kinase
-
-
?
ATP + CREB-binding protein
ADP + phosphorylated CREB-binding protein
show the reaction diagram
-
-
-
-
?
ATP + cyclin H protein
ADP + cyclin H phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + Dab1 protein
ADP + Dab1 phosphoprotein
show the reaction diagram
ATP + dephosphin
ADP + phosphorylated dephosphin
show the reaction diagram
ATP + DNA polymerase alpha
ADP + phosphorylated DNA polymerase alpha
show the reaction diagram
-
-
-
-
?
ATP + DNA polymerase sigma
ADP + phosphorylated DNA polymerase sigma
show the reaction diagram
-
-
-
-
?
ATP + E2F1 protein
ADP + E2F1 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + early mitotic inhibitor 1 protein
ADP + early mitotic inhibitor 1 phosphoprotein
show the reaction diagram
ATP + ErbB2
ADP + phosphorylated ErbB2
show the reaction diagram
ATP + ErbB3
ADP + phosphorylated ErbB3
show the reaction diagram
ATP + estrogen receptor
ADP + phosphorylated estrogen receptor
show the reaction diagram
-
Cdk2 phosphorylation at Ser104 and Ser106
-
-
?
ATP + eukaryotic elongation factor 2
ADP + phosphorylated eukaryotic elongation factor 2
show the reaction diagram
ATP + ezrin
ADP + phosphorylated ezrin
show the reaction diagram
-
phosphorylation by cdk5 at Thr235 in the NH2-terminal region and consequent dissociation of Rho GDP dissociation inhibitor from an ezrin/Rho-GDI complex
-
-
?
ATP + glucocorticoid receptor
ADP + phosphorylated glucocorticoid receptor
show the reaction diagram
-
-
-
-
?
ATP + HHASPRK
ADP + HHAS(P)PRK
show the reaction diagram
-
-
-
-
?
ATP + HHASPRK
ADP + phosphorylated HHASPRK
show the reaction diagram
-
-
-
-
?
ATP + histone 1
ADP + phosphorylated histone 1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
ATP + histone H1
ADP + phosphorylated steroid histone H1
show the reaction diagram
-
-
-
-
?
ATP + histone H1-derived peptide
ADP + histone H1-derived peptide phosphate
show the reaction diagram
-
-
-
-
?
ATP + histone H3 protein
ADP + histone H3 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + human cytomegalovirus tegument protein pp65
ADP + phosphorylated human cytomegalovirus tegument protein pp65
show the reaction diagram
-
-
-
-
?
ATP + huntingtin
ADP + phosphorylated huntingtin
show the reaction diagram
-
-
-
-
?
ATP + Mcm3
ADP + phosphorylated Mcm3
show the reaction diagram
-
-
-
-
?
ATP + Mcm4
ADP + phosphorylated Mcm4
show the reaction diagram
-
-
-
-
?
ATP + Med13 protein
ADP + Med13 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + MEK1
ADP + phosphorylated MEK1
show the reaction diagram
ATP + MEP50 protein
ADP + MEP50 phosphoprotein
show the reaction diagram
ATP + Munc-18
ADP + phosphorylated Munc-18
show the reaction diagram
ATP + NF-H
ADP + phosphorylated NF-H
show the reaction diagram
ATP + NF-M
ADP + phosphorylated NF-M
show the reaction diagram
ATP + NR1 receptor
ADP + phosphorylated NR1 receptor
show the reaction diagram
ATP + NR2 receptor
ADP + phosphorylated NR2 receptor
show the reaction diagram
ATP + Orc2
ADP + phosphorylated Orc2
show the reaction diagram
-
-
-
-
?
ATP + Orc6
ADP + phosphorylated Orc6
show the reaction diagram
-
-
-
-
?
ATP + p35 protein
ADP + p35 phosphoprotein
show the reaction diagram
-
a nuclear transcription factor, Cdk5-p25 phosphorylates p53 on Ser15, Ser33, and Ser44
-
-
?
ATP + parkin
ADP + phosphorylated parkin
show the reaction diagram
ATP + PKTPKKAKKL
ADP + PKpTPKKAKKL
show the reaction diagram
ATP + pocket protein p107
ADP + phosphorylated pocket protein 107
show the reaction diagram
ATP + pocket protein p130
ADP + phosphorylated pocket protein 130
show the reaction diagram
ATP + polymerase II C-terminal domain
ADP + phosphorylated polymerase II C-terminal domain
show the reaction diagram
Q140014
-
-
-
?
ATP + progesterone receptor
ADP + phosphorylated progesterone receptor
show the reaction diagram
ATP + promyelocytic leukemia zinc finger
ADP + phosphorylated promyelocytic leukemia zinc finger
show the reaction diagram
-
can also be phosphorylated by CDK1 albeit in a less efficient fashion than by CDK2
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + Rb peptide
ADP + Rb phosphopeptide
show the reaction diagram
-
from retinoblastoma-associated protein
-
-
?
ATP + replication factor C
ADP + phosphorylated replication factor C
show the reaction diagram
-
-
-
-
?
ATP + retinoblastoma protein
ADP + phosphorylated retinoblastoma protein
show the reaction diagram
ATP + retinoblastoma protein
ADP + retinoblastoma phosphoprotein
show the reaction diagram
ATP + RNA polymerase II
ADP + phosphorylated RNA polymerase II
show the reaction diagram
ATP + RNA polymerase II C-terminal domain
ADP + phosphorylated RNA polymerase II C-terminal domain
show the reaction diagram
ATP + RNA polymerase II C-terminal domain protein
ADP + RNA polymerase II C-terminal domain phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + RNA polymerase II carboxy-terminal domain
ADP + phosphorylated RNA polymerase II carboxy-terminal domain
show the reaction diagram
-
CDK8
-
-
?
ATP + RXL motif-containing peptide
ADP + RXL motif-containing phosphopeptide
show the reaction diagram
-
peptide sequence corresponding to amino acids 866-880 of RNA polymerase II C-terminal domain. Substrate phosphorylation by CDK6 with K-cyclin from Kaposi sarcoma herpesvirus, but addition of this peptide significantly reduces substrate phosphorylation by cyclin E-CDK2 and cyclin D2-CDK6
-
-
?
ATP + SCR-1
ADP + phosphorylated SCR-1
show the reaction diagram
ATP + SIRT2
ADP + phosphorylated SIRT2
show the reaction diagram
-
-
-
-
?
ATP + SMAD protein
ADP + SMAD phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
substrate of CDK5
-
-
?
ATP + STAT3 protein
ADP + STAT3 phosphoprotein
show the reaction diagram
-
Cdk5 phosphorylates at Ser727
-
-
?
ATP + steroid receptor coactivator-1
ADP + phosphorylated steroid receptor coactivator-1
show the reaction diagram
-
-
-
-
?
ATP + steroidogenic factor 1
ADP + phosphorylated steroidogenic factor 1
show the reaction diagram
-
also known as Ad4BP, systematic name NR5A1, the phosphorylation site is at Ser203
-
-
?
ATP + T-cell protein tyrosine phosphatase
ADP + phosphorylated T-cell protein tyrosine phosphatase
show the reaction diagram
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + Tau protein
ADP + Tau phosphoprotein
show the reaction diagram
ATP + tumor suppressor Rb
ADP + phosphorylated tumor suppressor Rb
show the reaction diagram
-
-
-
-
?
ATP + VGCC
ADP + phosphorylated NR1 receptor
show the reaction diagram
ATP + Wee1A
ADP + phosphorylated Wee1A
show the reaction diagram
ATP + [elongation factor 2]
ADP + [elongation factor 2]phosphate
show the reaction diagram
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
-
-
-
-
?
ATP + axonal cytoskeleton protein
ADP + phosphorylated axonal cytoskeleton protein
show the reaction diagram
-
regulated by integrin alpha1beta1
-
-
?
ATP + bloom syndrome helicase
ADP + phosphorylated bloom syndrome helicase
show the reaction diagram
-
-
-
-
?
ATP + BRCA2
ADP + phosphorylated BRCA2
show the reaction diagram
-
phosphorylates at Ser3291, phosphorylation reaches maximal levels in G2/M
-
-
?
ATP + c-Jun N-terminal kinase 3
ADP + phosphorylated c-Jun N-terminal kinase 3
show the reaction diagram
-
i.e. JNK3, phosphorylation inhibits JNK3 and leads to reduced phosphorylation of c-jun and to reduced apoptosis
-
-
?
ATP + Cdc20
ADP + phosphorylated Cdc20
show the reaction diagram
-
Cdk phosphorylation affects interaction of Cdc20 with Mad2 and the anaphase-promoting complex-cyclosome in HeLa cells
-
-
?
ATP + CDK1
ADP + phosphorylated CDK1
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK1
-
-
?
ATP + Cdk1
ADP + phosphorylated Cdk2
show the reaction diagram
-
Cdk7
-
-
?
ATP + cdk2
ADP + phosphorylated cdk2
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK2
-
-
?
ATP + Cprk
ADP + phosphorylated Cprk
show the reaction diagram
-
i.e. Cdk5/p35-regulated kinase
-
-
?
ATP + Dab1 protein
ADP + Dab1 phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + dephosphin
ADP + phosphorylated dephosphin
show the reaction diagram
-
Cdk5 regulates endocytosis involving dephosphin activity, overview
-
-
?
ATP + early mitotic inhibitor 1 protein
ADP + early mitotic inhibitor 1 phosphoprotein
show the reaction diagram
-
i.e. Emi1, is phosphorylated by CDKs in mitotic but not S-phase cell extracts
-
-
?
ATP + ErbB2
ADP + phosphorylated ErbB2
show the reaction diagram
-
phosphorylation of the neuregulin receptor by Cdk5 is involved in regulation of neuregulin
-
-
?
ATP + ErbB3
ADP + phosphorylated ErbB3
show the reaction diagram
-
phosphorylation of the neuregulin receptor by Cdk5 is involved in regulation of neuregulin
-
-
?
ATP + eukaryotic elongation factor 2
ADP + phosphorylated eukaryotic elongation factor 2
show the reaction diagram
-
phosphorylation on Ser595 by Cdk2
-
-
?
ATP + histone H1
ADP + phosphorylated steroid histone H1
show the reaction diagram
-
-
-
-
?
ATP + MEK1
ADP + phosphorylated MEK1
show the reaction diagram
-
Cdk5 regulates the ERK1/2 pathway through phosphorylation of MEK1, overview
-
-
?
ATP + MEP50 protein
ADP + MEP50 phosphoprotein
show the reaction diagram
-
a PRMT5 co-regulatory factor
-
-
?
ATP + Munc-18
ADP + phosphorylated Munc-18
show the reaction diagram
-
involved in regulation of exocytosis involving SNARE proteins, Munc-18 is required for mediating secretory responsesoverview
-
-
?
ATP + NF-H
ADP + phosphorylated NF-H
show the reaction diagram
-
neurofilament protein that correlates neurit outgrowth, phosphorylation at the KSP repeats, regulated by the myelin-associate glycoprotein
-
-
?
ATP + NF-M
ADP + phosphorylated NF-M
show the reaction diagram
-
neurofilament protein, phosphorylation at the KSP repeats, regulated by the myelin-associate glycoprotein
-
-
?
ATP + NR1 receptor
ADP + phosphorylated NR1 receptor
show the reaction diagram
-
involved in synaptic transmission, overview
-
-
?
ATP + NR2 receptor
ADP + phosphorylated NR2 receptor
show the reaction diagram
-
involved in synaptic transmission, phosphorylation of Ser1232 on the A subunit upregulates NMCAR activity, overview
-
-
?
ATP + p35 protein
ADP + p35 phosphoprotein
show the reaction diagram
-
a nuclear transcription factor, Cdk5-p25 phosphorylates p53 on Ser15, Ser33, and Ser44
-
-
?
ATP + parkin
ADP + phosphorylated parkin
show the reaction diagram
-
Ser-131 located at the linker region of parkin is the major Cdk5 phosphorylation site, phosphorylation by Cdk5 decreases the auto-ubiquitylation of parkin, parkin S131A mutant has 40% lower phosphorylation levels in vivo than wild-type parkin
-
-
?
ATP + pocket protein p107
ADP + phosphorylated pocket protein 107
show the reaction diagram
-
hyperphosphorylation by CDK/cyclin contributes to the transactivation of genes with functional E2F-binding sites, including growth and cell-cycle regulators, i.e. c-myc, Rb protein, cdc2, cyclin E, and cyclin A, and genes encoding proteins required for nucleotide and DNA biosynthesis
-
-
?
ATP + pocket protein p130
ADP + phosphorylated pocket protein 130
show the reaction diagram
-
hyperphosphorylation by CDK/cyclin contributes to the transactivation of genes with functional E2F-binding sites, including growth and cell-cycle regulators, i.e. c-myc, Rb protein, cdc2, cyclin E, and cyclin A, and genes encoding proteins required for nucleotide and DNA biosynthesis
-
-
?
ATP + polymerase II C-terminal domain
ADP + phosphorylated polymerase II C-terminal domain
show the reaction diagram
Q140014
-
-
-
?
ATP + progesterone receptor
ADP + phosphorylated progesterone receptor
show the reaction diagram
ATP + retinoblastoma protein
ADP + phosphorylated retinoblastoma protein
show the reaction diagram
ATP + retinoblastoma protein
ADP + retinoblastoma phosphoprotein
show the reaction diagram
-
a tumor suppressor protein
-
-
?
ATP + RNA polymerase II
ADP + phosphorylated RNA polymerase II
show the reaction diagram
-
CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II
-
-
?
ATP + RNA polymerase II C-terminal domain
ADP + phosphorylated RNA polymerase II C-terminal domain
show the reaction diagram
-
phosphorylation by Cdk7 and Cdk9, phosphorylation at serine residues 2 and 5
-
-
?
ATP + RNA polymerase II C-terminal domain protein
ADP + RNA polymerase II C-terminal domain phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + SCR-1
ADP + phosphorylated SCR-1
show the reaction diagram
-
Cdk2-cyclin A, phosphorylation at Lys5 regulates SCR-1 interaction with the progesterone receptor
-
-
?
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
substrate of CDK5
-
-
?
ATP + STAT3 protein
ADP + STAT3 phosphoprotein
show the reaction diagram
-
Cdk5 phosphorylates at Ser727
-
-
?
ATP + T-cell protein tyrosine phosphatase
ADP + phosphorylated T-cell protein tyrosine phosphatase
show the reaction diagram
-
phosphorylation of the two splicing varaints TC45 and TC48 at Ser304 in a cell cycle-dependent manner, optimally in mitosis, overview
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + Tau protein
ADP + Tau phosphoprotein
show the reaction diagram
-
Cdk5-p25 has a stronger Tau-phosphorylating activity than Cdk5-p35 in neurons
-
-
?
ATP + VGCC
ADP + phosphorylated NR1 receptor
show the reaction diagram
-
a voltage-dependent calcium channel, phosphorylation within the intracellular loop of the channel inhibiting interaction with SNARE proteins, SNAP-25, and synaptotagmin I required for neurotransmitter release, overview
-
-
?
ATP + Wee1A
ADP + phosphorylated Wee1A
show the reaction diagram
-
phosphorylation at S123, S53, and S121 promotes binding of Wee1A by beta-TrCP, the beta-transducin repeat-containing protein, which is the substrate recognition component of the ubiquitin ligase, leading to proteasomal degradation of Wee1A, overview
-
-
?
ATP + [elongation factor 2]
ADP + [elongation factor 2]phosphate
show the reaction diagram
-
the enzyme phosphorylates Ser595. Ser595 phosphorylation varies during the cell cycle and is required for efficient Thr56 phosphorylation (by elongation factor 2 kinase) in vivo
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cyclin
-
cyclin A
-
cyclin B
-
cyclin B1
-
required regulatory subunit of CDKs
-
cyclin C
-
cofactor of CDK3
-
cyclin D
-
cyclin D1
-
cyclin D2
-
cyclin D3
-
cyclin E
-
cyclin E2
-
cofactor of CDK3
-
cyclin H
-
cofactor of CDK7
-
cyclin K
-
-
-
cyclin L
-
cofactor of CDK11
-
cyclin T
-
cyclin V
-
regulatory subunit of CDK6
-
additional information
-
viral K-cyclin has a much longer half-life compared to cellular cyclins because it lacks the PEST degradation sequence, the viral K-cyclin can substitute the cellular cyclins in binding to the cellular CDKs, which is important for the virus development
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-cis-5,7-dihydroxyphenyl-8-[4-(3-hydroxy-1-methyl)piperidinyl]-4H-1-benzopyran-4-one
-
-
(1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
-
-
(2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
-
-
(2R)-2-{[9-(propan-2-yl)-6-({[4-(pyridin-2-yl)phenyl]methyl}amino)-9H-purin-2-yl]amino}butan-1-ol
-
-
(2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
-
-
(2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)methanol
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
-
41% inhibition at 0.01 mM
(3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
-
-
(3Z)-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is above 0.016 mM
(3Z)-3-[2-(4-bromophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.012 mM
(3Z)-5-bromo-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.030 mM
(3Z)-5-bromo-3-[2-(4-fluorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.029 mM
(3Z)-5-bromo-3-[2-(4-methylphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.029 mM
(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)hydrazine trihydrochloride
-
-
(4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(5Z)-2-(benzylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(butylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(cyclopropylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(methoxyamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(methylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(phenylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2,6-dichlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-bromobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-chlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-methoxybenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-phenylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-pyridin-2-ylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(3-hydroxy-2-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(3-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(pyridin-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[methyl(thiophen-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-2-methoxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R,2S)-2-phenylcyclopropyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1S)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-ethoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-methoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(3-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(3-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-bromophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-methoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethyl)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-[(2-thiophen-2-ylethyl)amino]-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-[(thiophen-2-ylmethyl)amino]-1,3-thiazol-4(5H)-one
-
-
(R)-roscovitine
1,2-di(2-pyridyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
1,2-dimethyl-1H-pyrazolo[3,4-c]pyridazine
-
-
1,25-dihydroxyvitamin D3
-
inhibition of CDK2 activity by 1,25-dihydroxyvitamin D3 is associated with decreased T160 phosphorylation, a residue whose phosphorylation in the nucleus is essential for CDK2 activity. 1,25-dihydroxyvitamin D3 increases the stability of the cyclin-dependent kinase inhibitor p27KIP1. Ectopic expression of cyclin E is sufficient to overcome 1,25-dihydroxyvitamin D3-mediated cytoplasmic mislocalization of CDK2 and all antiproliferative effects of 1,25-dihydroxyvitamin D3, yet endogenous levels of cyclin E or binding to CDK2 are not affected by 1,25-dihydroxyvitamin D3. Targeting CDK2 to the nucleus of 1,25-dihydroxyvitamin D3-sensitive cancer cells blocked G1 accumulation and growth inhibition by 1,25-dihydroxyvitamin D3
1-(1-acetylpiperidin-4-yl)-8-(cyclopentylamino)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)-3-ethylurea
-
-
1-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)-3-phenylurea
-
-
1-(5-cyclobutyl-thiazol-2-yl)-3-isoquinolin-5-yl-urea
-
competitive inhibitor
1-acetyl-3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
1-amino-3H-dibenzo[f,h]pyrazolo[3,4-c]cinnoline
-
-
1-benzyl-8-(cyclopentylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
1-methyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-2-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-3-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-4-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(phenylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(morpholin-4-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(piperidin-1-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[3-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[4-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[4-(methylsulfonyl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-NMPP1
-
inhibits Cdk7, selective inhibition of Cdk7 in G1 prevents activation but not formation of Cdk2/cyclin complexes and delays S phase. Inhibiting Cdk7 in G2 blocks entry to mitosis and disrupts Cdk1/cyclin B complex assembly
1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]-N,N-dimethyl-L-prolinamide
-
-
2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(3-chloro-4-piperazin-1-yl-phenylamino)-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-[(3,4-dimethoxyphenyl)amino]-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one
-
-
2-[(3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-1-yl)methoxy]ethanol
-
-
2-[(4-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
-
-
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-1-(methylsulfanyl)-2-oxoethanol
-
-
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
-
-
2-[2-(3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-1-yl)ethoxy]ethanol
-
-
2-[4-(4-acetyl-piperazin-1-yl)-phenylamino]-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
3-acetamide-1-acetyl-4,5-diphenyl-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-acetamide-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-1-benzyl-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4,5-bis(p-aminophenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-methoxyphenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-nitrophenyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4,5-bis(p-tert-butylphenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-trifluoromethylphenyl)-1H-pyrazolo-[3,4-c]pyridazine
-
-
3-amino-4,5-di(2-furyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-(2-furyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-methyl-4-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-isopropyl-5(R)-(2-hydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5(R)-[1-(hydroxymethyl)propyl]amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5,7-di[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(2,3-dihydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(2-aminoethyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(2-hydroxy-2-methylpropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(2-hydroxyethyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(3-amino-2-hydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(4-methoxybenzyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(N-morpholinyl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(piperazin-1-yl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(thiomorpholinyl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(trans-2-aminocyclohexyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-(trans-4-aminocyclohexyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-methylsulfanyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-methylsulfonyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-[2-(2-hydroxyethyl)piperidin-1-yl]-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-[2-(dimethylamino)ethyl]amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-5-[4-(2-hydroxyethyl)piperazin-1-yl]-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
3-[[(2,2-dioxido-1,3-dihydro-2-benzothien-5-yl)amino]methylene]-5-(1,3-oxazol-5-yl)-1,3-dihydro-2H-indol-2-one
-
-
3-[[4-([[amino(imino)methyl]amino]sulfonyl)anilino]methylene]-2-oxo-2,3-dihydro-1H-indole
-
-
4-(1,3-benzothiazol-2-yl)-N-(1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(2-fluoroethyl)thiophene-2-sulfonamide
-
poor inhibition of cdk5/p25
4-(1,3-benzothiazol-2-yl)-N-(4,5-dimethyl-1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(4-methylpyridin-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(5-hydroxypyridin-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(pyridin-2-ylmethyl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-hydroxythiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-[5-(morpholin-4-yl)pyridin-2-yl]thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
binds to Ile10 and Asp86 in the active site of cdk2
4-(1,4-dioxo-1,4-dihydro-naphthalen-2-ylamino)-N-(2-hydroxy-ethyl)-benzenesulfonamide
-
-
4-(1-ethyl-2-methyl-1H-imidazol-5-yl)-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-(6-acetyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
poor inhibition of cdk2/cyclin E
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-benzenesulfonamide
-
-
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2,3-dihydroxypropyl)-benzenesulfonamide
-
-
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2-hydroxyethyl)benzenesulfonamide
-
-
4-(6-chloro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-fluoro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-methyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-nitro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-chloro-N-(cis-3-[4-[(naphthalen-1-ylacetyl)amino]-1H-imidazol-1-yl]cyclobutyl)benzamide
-
-
4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
-
4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]-N-methylbenzenesulfonamide
-
-
4-[2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]benzenesulfonamide
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-(4-[[3-(1,3-oxazetidin-3-yl)propyl]sulfonyl]phenyl)pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(propylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-[(tetrahydrofuran-2-ylmethyl)sulfonyl]phenyl]pyrimidin-2-amine
-
-
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carbaldehyde
-
-
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
-
4-[4-(8-cyclopentyl-7-oxo-5-trifluoromethyl-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
-
4-[7-(4-chloro-3-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
-
-
4-[7-(4-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
-
poor inhibition of cdk2/cyclin E
4-[[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]amino]-N-(1,3-thiazol-2-yl)benzenesulfonamide
-
-
4-[[(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)methyl]amino]-N-(2-pyridinyl)benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)-N-methylbenzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-methylbenzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-[3-(1-methylethoxy)propyl]benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
4-[[4-(1-cyclopentyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1-cyclopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1-ethyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-dimethylbenzamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(2-hydroxypropyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-1,3-thiazol-2-ylbenzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenol
-
-
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzamide
-
29% inhibition at 0.001 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
-
33% inhibition at 0.01 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-dimethylbenzamide
-
49% inhibition at 0.1 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]benzamide
-
-
5,6-dichloro-1-beta-D-ribofuranosyl benzimidazole
-
cdk9 inhibitor
5,6-dichloro-1-beta-D-ribofuranosyl-benzimidazole
-
-
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole
-
specific CDK7 and 9 inhibition drives resolution of neutrophil-dominant inflammation
5-fluoro-6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6,7-dimethoxy-N-(3hydroxyphenyl)quinazolin-4-amine
-
-
6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6,8-dimethyl-N-[4-[4-(methylsulfonyl)piperazin-1-yl]phenyl]-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6-(cyclohexylmethoxy)-N2-(3-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-(4-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]pyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[4-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
-
6-acetyl-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-bromo-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-chloro-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-dimethylamino purine
-
potent inhibitor of CDK1/cyclin B
8-(1-ethyl-propyl)-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-(benzylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclohexylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
8-(cyclohexylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(2-hydroxyethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(4-sulfamoylphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(pyridin-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-phenyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-hydroxy-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-methyl-1-(1-methylpiperidin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-[1-(dimethylamino)propan-2-yl]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-[2-(dimethylamino)ethyl]-N-1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-cyclopentyl-2-(4-morpholin-4-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-5-trifluoromethyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperidin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-[1,4]diazepan-1-yl-phenylamino)-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3,3-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3,5-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3-hydroxy-pyrrolidin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-{4-[4-(3-hydroxy-propyl)-piperidin-1-yl]-phenylamino}-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5,6-dimethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-ethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-morpholin-4-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-piperidin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid methyl ester
-
-
8-cyclopentyl-6-ethyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-6-fluoro-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-ethyl-2-[4-(4-methylpiperazin-1-yl)phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-isopropyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-[(1-acetylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-ethylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-hydroxyethyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-[(3-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-bromobenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[4-(acetylamino)benzyl]amino]-1-methyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
actinomycin D
-
is less effective than 1-NMPP1 at inhibiting Cdk2 T loop phosphorylation
aloisine-A
-
-
alsterpaullone
aminopurvalanol
-
-
AMP
-
competitive inhibitor
anilinopyrimidine 32
-
-
apigenin
-
a flavonoid inhibitor of CDK6, CDK5, and CDK1
arylazopyrazole 31b
-
-
BMS-387032
-
-
BS-181
butyrolactone-1
-
-
CDK inhibitory proteins
-
members of the family of CDK inhibitory proteins, e.g. INK4 proteins, overview, CKIs may play a role as regulators in neointimal hyperplasia
-
Cdk2 inhibitor II
-
-
Cdk2DN
-
inhibition of Cdk2, induces phosphorylation of ataxia-telangiectasia mutated substrates
-
Cdk4/'6 Inhibitor IV
-
-
chrysin
-
a flavonoid inhibitor of CDK6, CDK5, and CDK1
CIP (154-279)
-
-
-
Cks1
-
Cks 1 protein inactivates Cdk2, activation of Chk1 leads to inactivation of Cdk2 by promoting phosphorylation-dependent turnover of the Cdk activating phosphatase Cdc25A
-
cyclin D1
-
inhibits the association and activation of androgen receptor by CDK6
-
cyclin-dependent kinase inhibitor p27KIP1
-
-
-
deoxyvariolin B
-
-
dinaciclib
-
-
DN-CDK2
-
suppresses CDK2 activity and partially increases erlotinib sensitivity
-
E2F1 peptide
-
81PALGRPPVKRRLDLE95
-
erlotinib
ethyl 4-[[1-methyl-3-(methylcarbamoyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl]amino]piperidine-1-carboxylate
-
-
ethyl [2-([[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]amino)-1,3-thiazol-4-yl]acetate
-
-
FAALS
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
fascaplysin
-
CDK4- and CDK6-specific inhibitor
fisetin
-
a flavonol inhibitor of CDK6, CDK5, and CDK1, binding structure with CDK6 involving V101, E61, K43, D163, and E99 of CDK6, overview
flavopiridol
ginsenoside F1
-
noncompetitive inhibition
ginsenoside Rb1
-
noncompetitive inhibition
ginsenoside Re
-
noncompetitive inhibition
ginsenoside Rf
-
noncompetitive inhibition
ginsenoside Rg1
-
noncompetitive inhibition
ginsenoside Rg2
-
noncompetitive inhibition
ginsenoside Rh1
-
noncompetitive inhibition
H1PAla
-
noncompetitive inhibitor
-
H1PPO4
-
noncompetitive inhibitor
-
hymenialdisine
-
-
IkappaBalpha
-
human protein, competes with INK4 proteins for binding sites on CDK4, CDK4 is bound at the N-terminal ankyrin repeats, while the C-terminal ankyrin repeats bind NF-kappaB, structure analysis
-
indirubin 3'-monoxime
-
-
indirubin-3'-monoxime
indirubin-3'-oxime
-
-
indirubin-5-sulfonic acid
-
-
INK4 proteins
-
inhibit CDK4
-
insulin-like growth factor binding protein-3
-
decreases the phosphorylation activity of CDK2 and CDK4
-
isopentenyladenine
kaempferol
-
a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1
kenpaullone
-
78% inhibition of CDK2 at 0.01 mM
KSLNRPFPDKIPELK
-
-
LAALS
-
; five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
LDC000067
LiCl
-
slight inhibition of T231 phosphorylation by p25-Cdk5 kinase complex
luteolin
-
a flavonoid inhibitor of CDK5 and CDK1
meridianin A
-
-
meridianin G
-
-
meriolin
-
-
meriolin 1
-
-
meriolin 2
-
-
meriolin 3
-
-
Myt1
-
Cdk1 inhibitor
-
N-(1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]azetidin-3-yl)acetamide
-
-
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(2-methylpropyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
N-(2-methoxyethyl)-4-[[4-(1,2,4-trimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
N-(3-{[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)-4-{[(2E)-4-(dimethylamino)but-2-enoyl]amino}benzamide
-
-
N-(4-[4-[(2-methoxyethyl)sulfonyl]piperazin-1-yl]phenyl)-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-amine
-
-
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-(5-nitro-1H-indazol-3-yl)-2-phenylacetamide
-
-
N-(6-amino-pyrimidin-4-yl)-sulfanilic acid amide
-
-
N-1-dimethyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-benzyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-cyclohexyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-methyl-4-[[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]amino]benzenesulfonamide
-
-
N-methyl-[4-[2-(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)hydrazino]phenyl]methanesulfonamide
-
-
N-[(3R)-1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]pyrrolidin-3-yl]acetamide
-
-
N-[(9bR)-5-oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-alpha]isoindol-9-yl]-N'-pyridin-2-yl urea
-
-
N-[(9bR)-5-oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-alpha]isoindol-9-yl]-N'-{5-[(2S)-pyrrolidin-2-yl]-1H-pyrazol-3-yl urea
-
-
N-[2-(1-aminohydrazino)ethyl]-4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
N-[2-(dimethylamino)ethyl]-4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
-
N-[4-(4-[[(diethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(4-[[(dimethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(4-[[2-(dimethylamino)ethyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(benzylsulfonyl)phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-[4-[(2-methoxyethyl)sulfonyl]phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
-
-
N-[5-(2,5-dioxoimidazolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(2-oxopiperidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(2-oxopyrrolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(dibutylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(diethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(dipropylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(ethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N2-(3-bromophenyl)-6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
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N2-(3-bromophenyl)-6-(cyclohexylmethoxy)pyrimidine-2,4-diamine
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N4-(6-aminopyrimidin-4-yl)-sulfanilamide
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competitive inhibitor
NU-2058
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NU-6027
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NU6102
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highly potent and selective ATP-competitive inhibitor of CDK2
Olomoucine
olomoucine II
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p15Ink4b
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INK4 protein
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p16Ink4a
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p18
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wild-type and D76A mutant human INK4 protein, the mutant is only slightly inhibitory, p18 competes with IkappaBalpha for binding sites on CDK4, structure analysis
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p18Ink4c
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INK4 protein
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p19Ink4d
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INK4 protein
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p21
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p21 protein
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i.e. Cip1 or Waf1, a Cdk-inhibitor
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p21CIP
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as recombinant GST-tagged protein
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p21Cip1
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inhibits phosphorylation of tumor suppressor Rb
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p21Clp1
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forms a ternary complex with and is negatively regulated by p21Cip1, but not by its truncated fragment p21Cip1-D3
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p21v1
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endogenous CDK inhibitor
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p21v2
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endogenous CDK inhibitor
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p21WAF1/CIP1
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specific Cdk inhibitor, efficiently prevents etoposide-induced apoptotic cell death
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p27
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P276-00
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p27Kip1
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p27Kip1 cyclin-dependent-kinase inhibitor
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palbociclib
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PD-0332991
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PD183812
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PHA-848125
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PKF049-365
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pRb peptide
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866SNPPKPLKKLRFDIE880
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progesterone
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protopanaxatriol
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noncompetitive inhibition
purvalanol
purvalanol A
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purvalanol B
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specific inhibitor of CDK1, 2, 5, and 7
pyrazolopyridazine
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quercetin
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a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1
R547
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RBG-286147
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RO-3306
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roscovitine
RXL motif-containing peptide
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addition of this peptide significantly reduces substrate phosphorylation by cyclin E-CDK2 and cyclin D2-CDK6
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SCH-727965
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shRNA
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cdk5 shRNA is able to efficiently inhibit the expression of endogenous cdk5
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simvastatin
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inhibition of CDK2
siRNA
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SNS-032
staurosporine
SU-9516
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SU9516
TAACS
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; five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALD
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five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALE
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five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALS
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disrupts the cdk2/cyclin E complex
tranilast
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inhibition of CDK2 and CDK4
tumour suppressor p16INK4a
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-
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UCN-01
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variolin B
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Wee1
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Cdk1 inhibitor
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[(2R)-1-[[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]pyrrolidin-2-yl]methanol
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poor inhibition of cdk2/cyclin E
[8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-3-yl](4-methylpiperazin-1-yl)methanone
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additional information
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Cdc25A
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CDK-activating kinase
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the CDK-activating kinase (having three subunits, CDK7, cyclin H, and MAT1) plays a critical role in regulating cell cycle by mediating the activating phosphorylation of CDK1, CDK2, CDK4, and CDK6
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Cks2
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Cks 2 proteins activates Cdk2
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cyclin
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dependent on, forms complexes with cyclin A
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cyclin A
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cyclin B
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cyclin D1
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cyclin D2
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-
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cyclin D3
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cyclin E
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cyclin H
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activates Cdk7
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cyclin I
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-
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cyclin T
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CDK9 activating partner cyclin T1
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cyclin T1
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activates Cdk9
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dynein light chain 1
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interacts with cdk2 and enhances Cdk2 kinase activity in vivo, dynein light chain 1 accelerates the G1-S transition by enhancing the activity of Cdk2
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E2F1
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etoposide
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activity of Cdk2 selectively increases after 6-9 h and then continues to increase over the 24 h time course of etopside treatment
p25
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p34SEI-1
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i.e. TRIP-Br1, the protein binds directly to CDK4 and activates it at lower concentrations, but inhibits the enzyme at higher concentrations, p34SEI-1 has regulatory function, the binding is not affected by INK4 proteins p16 and p18, complex formation of CDK4, cyclin D2, p16, and p34SEI-1, p34SEI-1 has a LexA-mediated transactivation activity, determination of functional sequence units/fragments in the protein, overview
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p35
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p39
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p58
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regulatory subunit of CDK11
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progestin
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Protein phosphatase 2A
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PP2A, enhances CDK8 kinase activity in vitro for the RNA polymerase II carboxy-terminal domain but not for histone H3. PP2A enhancement of CDK8 is independent of RV-cyclin expression and likely plays a role in the normal regulation of CDK8
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RV-cyclin
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retroviral cyclin from Walleye dermal sarcoma virus, enhances CDK8 kinase activity in vitro for RNA polymerase II carboxy-terminal domain and histone H3. It is specific for cdk8, no activation of Cdk7 or Cdk9. The majority of the RV-cyclin structure is comprised of a cyclin box fold, which is responsible for binding to cyclin-dependent kinase-8. Two-hybrid interaction analysis in Saccharomyces cerevisiae strain Y190
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additional information
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