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PP2A inhibitor
Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM. -
HIV protease inhibitor
Darunavir Ethanolate (Prezista) is an HIV protease inhibitor. - Indinavir sulfate is a novel hydroxyaminopentane amide class of HIV-1 protease inhibitors.
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Apoptosis Activator
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells - Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
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HCV NS3/4A protease inhibitor
Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of NS3/4A protease polymorphisms. GS-9857 improves coverage against commonly encountered NS3 resistance-associated variants (RAVs). -
thrombin/factor Xa dual inhibitor
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity. -
NF-kB inhibitor/Proteasome activator
18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1). -
proteasome inhibitor
Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. -
MTP inhibitor
PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.
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Caspase/apoptosis activator
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively. -
cathepsin S inhibitor
Petesicatib is a cathepsin S inhibitor, used in research of immune diseases. - FABP4 Inhibitor is a cell-permeable biphenylazolo-oxyacetate that acts as a potent and selective inhibitor of adipocyte Fatty-Acid-Binding Protein (aFABP/aP2) by targeting its fatty acid-binding pocket (Ki = < 2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP's (Ki = 250 nM and 350 nM, respectively).
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HCV NS5B polymerase inhibitor
Deleobuvir (BI207127) was a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C
- 4-Butylresorcinol is a phenol derivative which can inhibit tyrosinase with IC50 of 11.27 μM.
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aldose reductase inhibitor
Ranirestat is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy. -
DPP-4 inhibitor
Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9. -
DPP-4 inhibitor
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. -
Aminopeptidase inhibitor
Bestatin methyl ester is a cell-permeable derivative of Bestatin which displays slightly stronger inhibition of neutral aminopeptidase than Bestatin, but has much weaker activity against basic aminopeptidase. -
Serine protease inhibitor
AAF-CMK is a serine protease inhibitor which irreversibly inhibits TPPII (tripeptidyl peptidase II), a giant protease which may substitute for some proteasome functions1, and reversibly inhibits Cln2 (TPPI). -
cathepsin C substrate
Gly-Phe-beta-naphthylamide is a cathepsin C substrate. The compound is described to accumulate inside lysosomes leading to their destruction. -
gamma-secretase inhibitor
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). -
neprilysin inhibitor
AHU-377 is an inhibitor of neprilysin with IC50 value of 5nM. - 25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types
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TACE/MMP inhibitor
(S,S)-TAPI-0 is an inhibitor of TACE (IC50 = 50-100 nM) as well as other matrix and membrane metalloproteases
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DPIV and DP8/9 inhibitor
DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively. -
HCV NS5A inhibitor
MK 8742, also known as Elbasvir, is a HCV NS5A inhibitor, which is an all-oral, interferon-free regimen for the treatment of HCV infection. -
TACE/MMP inhibitor
TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors.

