Activators & Inhibitors

CTPB is a potent activator of p300 activity, but not of PCAF (p300/CBP-associated factor). This compound has been shown to enhance p300 HAT-dependent transcriptional activation from in vitro assembled chromatin template. CTPB has also been noted to be a membrane-impermeable molecule that requires a carrier to move across the membrane barrier of cells.

Telaprevir inhibits the hepatitis C virus NS3-4A serine protease, leading to the block of viral polyprotein processing. This eventually leads to a decrease of viral RNA replication, HCV RNA levels, as well as and protein levels in the Con1 (genotype 1b) subgenomic HCV replicon cells. This occurs in a time- and dose-dependent manner.

Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with an IC50 of 0.2-3.5 nM.

VX-222 is a novel, potent and selective inhibitor of non-nucleoside polymerase of the hepatitis C virus (HCV) RNA-dependent RNA polymerase, with an IC50 range of 0.94-1.2 µM. VX-222 selectively inhibits the replication of both HCV1a and HCV1b.

BMS-790052 is a highly selective and highly potent inhibitor of hepatitis C virus (HCV) NS5A. The mean EC50 values of BMS-790052 are 50 and 9 pM for HCV genotype 1a and 1b replicons, respectively. BMS-790052 is inactive towards a panel of 10 RNA and DNA viruses, with EC50 higher than 10 µM.

Orally active protease inhibitor. Known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin.

PD 173074 inhibited the kinase activity of FGFR1 with an IC50 of 25 nM in vitro, while inhibiting Src, the receptors for insulin, epidermal growth factor (EGF) and PDGF, and several serine/threonine kinases with 1000-fold or higher IC50 values. PD 173074 was an ATP-competitive inhibitor of FGFR1, with a Ki of around 40 nM. PD 173074 inhibited autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50s in the range of 1-5 nM and 100-200 nM, respectively.

A-769662 is a potent, reversible activator of AMP-activated protein kinase (AMPK). AMPK is an αβγ heterotrimer and plays an important role in regulating cellular and whole-body metabolism. A-769662 only activates AMPK heterotrimers containing the β1 subunit. A-769662 activates AMPK through the β subunit carbohydrate-binding module and the γ subunit but not the AMP-binding sites. A-769662 stimulated partially purified rat liver AMPK with an EC50 of 0.8 µM and inhibited fatty acid synthesis in primary rat hepatocytes with an IC50 of 3.2 µM.

Immunosuppressant, related to FK-506, but without calcineurin inhibitory activity even when complexed to FK-506 binding protein. Selectively blocks signaling that leads to p70 S6 kinase activation (IC50 = 50 pM).