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YK-3-237

CAS No. : 1215281-19-8

MCE 站：YK-3-237

产品活性：YK-3-237 是一种 SIRT1 激活剂，靶向突变体 p53。YK-3-237 抑制三阴性乳腺癌细胞的增殖。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：Sirtuin

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 ?M, 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 ?M, 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 ?M, respectively.
YK-3-237 (0.01-10 ?M; 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.
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.

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