Chemicals & Small Molecules

Procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 µM). Also activates procaspase-7 in a less efficient manner (EC50 = 4.5 µM). Pro-apoptotic; induces apoptosis in both cancerous and non-cancerous cells dependent on procaspase-3 concentration (IC50 values are 0.003 - 1.41 and 5.02 - 9.98 µM respectively). PAC-1 had an IC50 value of 3 nM for induction of cell death, whereas in cells from adjacent normal tissue IC50 values of 3.2-8.5 µM were observed

Obatoclax, also known as GX15-070, is a novel Bcl-2 homology domain-3 (BH3) mimetic. It occupies a hydrophobic cleft within the BH3 binding groove of Bcl-2, antagonizing Bcl-2 and thus inducing apoptosis. Obatoclax inhibited primary acute myeloid leukemia (AML) progenitor cell proliferation with an average IC50 of 0.18 ± 0.07 µM, and it potently induced apoptosis in primary AML cells with an average IC50 of 3.6 ± 1.2 µM. Obatoclax overcomes Bcl-2-, Bcl-xL-, Bcl-w-, and Mcl-1-mediated resistance to BAX or BAK and to the proteasome inhibitor bortezomib.

BIIB021 is an orally available, synthetic small-molecule Hsp90 inhibitor. It binds in the ATP-binding pocket of Hsp90 (Ki = 1.7 ± 0.4 nM) and induces HER-2 degradation with an EC50 of 38 ± 10 nM in MCF-7 cells. It ncreases expression of the heat shock proteins Hsp90α and Hsp70, but has no effect on expression of the nonclient protein phosphatidylinositol 3-kinase p85 subunit. BIIB021 inhibits the proliferation of N87, MCF-7, and BT474 tumor cells with IC50 values of 0.06, 0.31, and 0.14 µM, respectively. It has significant antitumor activity in N87 stomach, BT474 breast, CWR22 prostate, U87 glioblastoma, SKOV3 ovarian, and Panc-1 pancreatic tumor xenograft models.

Potent inhibitor of protein phosphatases, especially the PP-1 and PP-2 classes, in numerous cell types. Non-phorbol type tumor promoter.

AICAR, also known as acadesine, is an adenosine regulating agent and AMPK activator. AICAR was found to activate AMP-activated protein kinase (AMPK) in skeletal muscle, inhibit acetyl-CoA carboxylase, reduce malonyl-CoA, and increase fatty acid oxidation and glucose uptake. Note: This product is not 5'-phosphorylated.

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.