Chemicals & Small Molecules

PCI-24781 (also known as CRA-024781) is a novel, broad spectrum inhibitor of HDACs that shows antitumor activity in vitro. PCI-24781 primarily targets HDAC1 (Ki = 7 nM). It also exhibits modest potenty toward HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.

PCI-24781 (also known as CRA-024781) is a novel, broad spectrum inhibitor of HDACs that shows antitumor activity in vitro. PCI-24781 primarily targets HDAC1 (Ki = 7 nM). It also exhibits modest potenty toward HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.

PCI-24781 (also known as CRA-024781) is a novel, broad spectrum inhibitor of HDACs that shows antitumor activity in vitro. PCI-24781 primarily targets HDAC1 (Ki = 7 nM). It also exhibits modest potenty toward HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.

Potent and oral inhibitor of histone deacetylase (HDAC), selective for class I, II and IV HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, with high tumor exposure and efficacy in mouse models of colorectal cancer.

Potent and oral inhibitor of histone deacetylase (HDAC), selective for class I, II and IV HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, with high tumor exposure and efficacy in mouse models of colorectal cancer.

Potent and oral inhibitor of histone deacetylase (HDAC), selective for class I, II and IV HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, with high tumor exposure and efficacy in mouse models of colorectal cancer.

SMI-4a is a potent inhibitor of Pim1 with IC50 = 17 -21 nM. It does not significantly inhibit other serine/threonine- or tyrosine-kinases. It induces G1 phase cell cycle arrest and induces apoptosis through the mitocondrial pathway. It downregulates c-myc and induces p27Kip1 expression. Inhibits PRAS40 phosphorylation and mTOR activity, as well as the mammalian target of rapamycin C1 (mTORC1) pathway. SMI-4a is a potential anti-cancer compound that blocks prostate cancer growth.

SMI-4a is a potent inhibitor of Pim1 with IC50 = 17 -21 nM. It does not significantly inhibit other serine/threonine- or tyrosine-kinases. It induces G1 phase cell cycle arrest and induces apoptosis through the mitocondrial pathway. It downregulates c-myc and induces p27Kip1 expression. Inhibits PRAS40 phosphorylation and mTOR activity, as well as the mammalian target of rapamycin C1 (mTORC1) pathway. SMI-4a is a potential anti-cancer compound that blocks prostate cancer growth.

TW-37 is a potent small-molecule inhibitor that attenuates Bcl-2 activation and inhibits multiple Bcl-2 family members including Bcl-xL and Mcl-1. TW-37 also inhibits in vivo and in vitro the activation of Jagged-1 and Notch-1.