YK-3-237

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型小分子 Sirtuin-1 (SIRT1) 激活剂，可减少突变体 53 的乙酰化，并对携带突变体 p53 的 TNBC 细胞表现出抗增殖作用。

A novel small molecule sirtuin-1 (SIRT1) activator that reduces acetylation of mutant 53 and exhibits anti-proliferative effects against TNBC cells carrying mutant p53; demonstrates proliferation inhibition in breast cancer cell panel with EC50 of 0.1-5 uM, also induces PARP-dependent apoptotic cell death and arrests the cell cycle at G2/M phase; enhances expression of α-SMA and fibronectin in cultured rat renal interstitial fibroblasts (NRK-49F).

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.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. Cell Viability Assay Cell Line:BT549, MDA-MB-468, HS578T, SUM149PT Concentration:0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time:24 hours Result:Reduced both the acetylation of K382 and the level of mtp53 in a dose-dependent manner in mtp53 TNBC cell lines.

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YK-3 237

Chromatin/Epigenetic

Sirtuin

Sirtuin

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1215281-19-8

372.18

C19H21BO7

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (268.69 mM)

B(C1=C(C=CC(=C1)C=CC(=O)C2=CC(=C(C(=C2)OC)OC)OC)OC)(O)O

B-[2-methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]-boronic acid

(-20℃)

With Ice Pack

≥ 2 years