YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.In Vitro: YK-3-237 exhibits the anti-proliferative activities toward most of the breast cancer cell lines tested at submicromolar concentration. YK-3-237 preferentially inhibits the proliferation of breast cancer cell lines carrying mtp53.
YK-3-237 inhibits the proliferation of triple-negative breast cancer (TNBC) HS578T, MDA-MB-453, SUM1315MO2, SUM149PT, BT549, MDA-MB-231, MDA-MB-436, MDA-MB-468, HCC1937 with IC50s of 0.160±0.043, 0.241±0.086, 0.253±0.028, 0.289±0.066, 0.353±0.017, 0.431±0.136, 0.501±0.062, 1.436±0.754, 5.031±2.010 μM, respectively.
YK-3-237 inhibits the proliferation of Luminal T47D, MCF7, and ZR-75-1 with IC50s of 1.573±0.370, 2.402±0.256, 3.822±0.967 μM, respectively.
YK-3-237 inhibits the proliferation of HER2 BT474 and SK-BR-3 with IC50s of 1.249±0.372 and 0.346±0.066 μM, respectively.
YK-3-237 (0.01-10 μM; 24 hours) deacetylates mtp53 in TNBC cell lines.
YK-3-237 is a potent activator of Sirt1, on the activation of renal interstitial fibroblasts using NRK-49F cells[2].
Exposure of cells to YK-3-237 also significantly reduces expression of α-SMA and fibronectin in a dose-dependent manner, with the maximum inhibition occurring at 10 μM[2].