YK-3-237 is a SIRT1 activator, specifically targets mutant p53 and curtails the growth of triple-negative breast cancer (TNBC) cells[1].
体外研究
YK-3-237 exhibits anti-proliferative effects on a broad range of breast cancer cell lines at submicromolar concentrations, showing a marked preference for halting the proliferation of those harboring mutant p53 (mtp53)[1].
YK-3-237 effectively impedes the growth of various TNBC cell lines, with IC50 values spanning from 0.160±0.043 µM to 5.031±2.010 µM, depending on the cell line[1].
YK-3-237 inhibits the proliferation of 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[1].
Otherwise, YK-3-237 also inhibits the proliferation of HER2 BT474 and SK-BR-3 with IC50s of 1.249±0.372 and 0.346±0.066 µM, respectively[1].
At concentrations ranging from 0.01 to 10 µM over 24 hours, YK-3-237 leads to the deacetylation of mtp53 in TNBC cell lines[1].
Moreover, YK-3-237 is affirmed as a robust Sirt1 activator in the context of renal interstitial fibroblasts, utilizing NRK-49F cells for experimentation[2].
Exposure to YK-3-237 results in a dose-dependent reduction of α-smooth muscle actin (α-SMA) and fibronectin expression, achieving maximal inhibition at 10 µM[2].
搜索
