YK-3-237

YK-3-237 is a chalcone derivative and an activator of sirtuin 1 (SIRT1).[1],[2] It inhibits colchicine binding to tubulin in a concentration-dependent manner and tubulin polymerization (IC50 = 31 μM) and induces microtubule loss in A-10 cells (EC50 = 16.5 μM).[1] YK-3-237 inhibits cell growth in a panel of leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate, and breast cancer cell lines (GI50s = <0.01-20.9 μM). It inhibits tube formation by human umbilical vein endothelial cells (HUVECs) when used at a concentration of 1 μM and inhibits functional angiogenesis in isolated rat aortic rings. YK-3-237 activates SIRT1 in a concentration-dependent manner and reduces acetylation of wild-type and mutant p53 in a SIRT1-dependent manner.[2] It also inhibits cell growth in panel of 9 triple-negative breast cancer (TNBC) cell lines (EC50s = 0.160-5.031 μM).

Reference:
[1]. Kong, Y., Wang, K., Edler, M.C., et al. A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent. Bioorg. Med. Chem. 18(2), 971-977 (2010).
[2]. Yi, Y.W., Kang, H.J., Kim, H.J., et al. Targeting mutant p53 by a SIRT1 activator YK-3-237 inhibits the proliferation of triple-negative breast cancer cells. Oncotarget 4(7), 984-994 (2013).