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(2R,2'R)-2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino[(2S)-1-oxo-4-phenylbutane-2,1-diyl]imino]]bis(3-phenylpropanoic acid)
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(2S,2'S)-2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino]]bis(3-methylbutanoic acid)
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(2S,2'S)-2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino]]bis(4-phenylbutanoic acid)
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(3S,4S,5S,6R)-2-([(2R,3S,4S,5S,6S)-3,5-dihydroxy-2-(hydroxymethyl)-6-methoxytetrahydro-2H-pyran-4-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol
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i.e. BJ-12-26-1, greatly reduces SKI-1 zymogen processing, and abolishes the processing of substrate SREBP-2
(3S,4S,5S,6R)-2-([(2S,3S,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol
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i.e. BJ-12-21-2, greatly reduces SKI-1 zymogen processing, and abolishes the processing of substrate SREBP-2
(R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
inhibits endogenous SREBP processing in Chinese hamster ovary cells. Compound down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In mice treated with the compound for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced
(S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
purified S-enantiomer
1-(4-[[2-(2-methoxyphenyl)ethyl](pyrrolidin-3-yl)carbamoyl]benzyl)piperidine-3-carboxamide
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2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino]]diacetic acid
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3,4-dichloroisocoumarin
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potent slow binding inhibitor, 100% inhibition by 0.05 mM
4-(2-aminoethyl benzene)sulfonyl fluoride
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i.e. AEBSF, competitive
4-(2-aminoethyl)-benzenesulfonyl fluoride
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4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
4-(2-azabicyclo[2.2.1]hept-2-ylmethyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-(6-azabicyclo[3.2.1]oct-6-ylmethyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-(benzyloxy)-N-[2-(2-chlorophenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-(benzyloxy)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-(benzyloxy)-N-[2-(3-chlorophenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-([[(1S,2S)-2-hydroxycyclohexyl]amino]methyl)-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-[(diethylamino)methyl]-N-[2-(2-ethoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-[(3R)-pyrrolidin-3-yl]benzamide
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4-[(diethylamino)methyl]-N-[2-(2-methylphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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4-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-pyrrolidin-3-ylbenzamide
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Ac-VFRSLK-4-(2-aminoethyl benzene)sulfonyl fluoride
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benzyl N-[(2-[(E)-[2-(2-oxo-2-[[(1S)-2-oxo-2-phenoxy-1-phenylethyl]amino]ethoxy)phenyl]diazenyl]phenoxy)acetyl]-L-phenylalaninate
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competitive. E-isomer is thermally stable
benzyl N-[(2-[(E)-[2-(2-[[(2S)-3-methyl-1-oxo-1-phenoxybutan-2-yl]amino]-2-oxoethoxy)phenyl]diazenyl]phenoxy)acetyl]-L-leucinate
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competitive. E-isomer is thermally stable
brefeldin A
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abrogates St-2 production
Ca2+
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inhibition above 3 mM
CuSO4
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complete inactivation at 1 mM
decanoyl-RRLL-chloromethylketone
the selective and cell-permeable small-peptide inhibitor inhibits the enzyme and leads to suppression of proliferation and metabolic activity of melanoma cells in vitro. The inhibitor induces classical apoptosis of melanoma cells in vitro and affects expression of several SKI-1 target genes including activating transcription factor 6. The compound induces cell death in an ATF6-independent manner
decanoyl-RVKR-chlorometylketone
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66% inhibition at 0.05 mM
dibenzyl (2R,2'S)-2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino]]bis(3-methylbutanoate)
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dibenzyl (2R,2'S)-2,2'-[(E)-diazene-1,2-diylbis[benzene-2,1-diyloxy(1-oxoethane-2,1-diyl)imino]]bis(3-phenylpropanoate)
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dithiothreitol
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partial inhibition at very high concentrations
ethanolamine
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supresses cleavage by dS1P
gabexate mesylate
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8% inhibition at 0.05 mM
N-(2-chlorobenzyl)-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide
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N-[(2-[(E)-[2-(2-[[(1S)-1-carboxy-2-methylpropyl]amino]-2-oxoethoxy)phenyl]diazenyl]phenoxy)acetyl]-L-leucine
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competitive. E-isomer is thermally stable
N-[2-(2,6-dichlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-chlorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-chlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-chlorophenyl)ethyl]-4-[[3-(2-methylphenyl)piperidin-1-yl]methyl]-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-fluorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-methoxyphenyl)ethyl]-4-(piperidin-1-ylmethyl)-N-pyrrolidin-3-ylbenzamide
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N-[2-(2-methoxyphenyl)ethyl]-4-[[3-(2-methylphenyl)piperidin-1-yl]methyl]-N-pyrrolidin-3-ylbenzamide
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N-[2-(3-chlorophenyl)ethyl]-4-(1-methylethoxy)-N-pyrrolidin-3-ylbenzamide
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N-[2-(4-chlorophenyl)ethyl]-4-[(diethylamino)methyl]-N-pyrrolidin-3-ylbenzamide
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palmitate
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supresses cleavage by dS1P
Pefabloc SC
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at high concentrations
PF429242
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inhibotor suppresses the formation of soluble (pro)renin receptor
PMSF
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12% inhibition at 0.05 mM
prosegment of SKI-1
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ZnSO4
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complete inactivation at 1 mM
1,10-phenanthroline
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complete inactivation at 5 mM
1,10-phenanthroline
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partial inhibition at very high concentrations
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
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inhibits SKI-1 and the autocatalytic generation of St-1
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
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EDTA
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complete inactivation at 10 mM
EDTA
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partial inhibition at very high concentrations
EGTA
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85% inactivation at 10 mM
EGTA
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partial inhibition at very high concentrations
PF-429242
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potent S1P inhibitor both in vitro and in cell-based assays, PF-429242 inhibits S1P-mediated processing of arenavirus arenavirus glycoprotein precursor protein
PF-429242
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active-site-directed inhibitor
additional information
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decanoyl-RVKR-chloromethylketone does not affect SKI-1-mediated processing; decanoyl-RVKR-chloromethylketone inhibition is selective to furin/PCs and does not affect SKI-1-mediated processing
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additional information
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SKI-1/S1P inhibition by overexpression of proSKI variants, results in reduced cholesterol synthesis and mRNA levels of the rate-limiting enzymes HMG-CoA reductase and squalene epoxidase in the cholesterol synthetic pathway. Inhibitory effect is maintained in the presence of homocysteine-induced endoplasmic reticulum stress. SKI-1/S1P inhibition also affects glycolysis and citric acid cycle
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additional information
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(Z-LL)2-chloromethylketone and PN1 have no effect on St-2 production. Overexpressed rSt-1 or rSt-2 impede ATF6 processing by SKI-1
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additional information
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not inhibited by Mn2+, 7B2 C-terminal peptide, ProSAAS235-244 peptide, ProSAAS235-246 peptide, trypsin inhibitor from bovine pancreas, trypsin inhibitor from soybean, Pefabloc SC (4-(2-aminoethyl) benzene sulphonyl fluoride), benzamidine, p-aminobenzamidine and chymostatin
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