YK-3-237

• CAT Number: M011459
• CAS Number: 1215281-19-8
• Molecular Formula: C19H21BO7
• Molecular Weight: 372.18
• Purity: ≥95%
• Synonyms: [2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxyphenyl)prop-1-enyl]phenyl]boronic acid
• InChI: InChI=1S/C19H21BO7/c1-24-16-8-6-12(9-14(16)20(22)23)5-7-15(21)13-10-17(25-2)19(27-4)18(11-13)26-3/h5-11,22-23H,1-4H3/b7-5+
• InChIKey: AKNGHUAJAODDJA-FNORWQNLSA-N
• SMILES: B(C1=C(C=CC(=C1)C=CC(=O)C2=CC(=C(C(=C2)OC)OC)OC)OC)(O)O

YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells[1].
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[1].
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[1].
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[1].
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[1].
YK-3-237 (0.01-10 µM; 24 hours) deacetylates mtp53 in TNBC cell lines[1].
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].

Reference

[1]. Yong Weon Yi, et al. Targeting mutant p53 by a SIRT1 activator YK-3-237 inhibits the proliferation of triple-negative breast cancer cells. Oncotarget. 2013 Jul;4(7):984-94.
 [Content Brief]

[2]. Murugavel Ponnusamy, et al. Activation of Sirtuin-1 Promotes Renal Fibroblast Activation and Aggravates Renal Fibrogenesis. J Pharmacol Exp Ther. 2015 Aug;354(2):142-51.
 [Content Brief]