CCT018159

CCT018159 is an ATP-competitive HSP90β inhibitor, with an IC₅₀ of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. CCT018159 induces cell cycle arrest and apoptosis in tumor cells, and inhibits invasion and angiogenesis. CCT018159 is applicable to cancer-related research^[1][2]. In Vitro:CCT018159 inhibits the growth of human cancer cell lines with a mean GI₅₀ of 5.3 μM, and its activity against HUVECs (GI₅₀ 0.87 μM) is stronger than that against most cancer cell lines^[1].
CCT018159 (24 h) induces characteristic molecular markers of HSP90 inhibition, including upregulation of HSP72, depletion of client proteins (C-RAF, CDK4, ERBB2, mutant B-RAF), and decreased phosphorylation level of ERK1/2 in human cancer cells, as well as modulates angiogenesis-related client proteins in HUVECs^[1].
CCT018159 (41 μM; 16-72 h) induces cell cycle arrest and apoptosis in SKMEL 5 melanoma cells^[1].
CCT018159 (0-4.4 μm; 24-48 h) inhibits the key functions of endothelial cells as well as invasion-related functions of tumor cells^[1].
CCT018159 (0.1-50 μM) reduces the viability of NCI-H295R cells in a dose-dependent manner, with an EC₅₀ of 11.5 μM^[2].