YK-3-237 is an activator of sirtuin-1 (SIRT1). YK-3-237 showed anti-proliferative activity toward triple-negative breast cancer, inducing G2/M cell cycle arrest and apoptosis. In a study on renal fibrosis, YK-3-237 caused enhanced expression of α-SMA and fibronectin, suggesting that long-term use of SIRT1 activators may increase the risk or progression of chronic kidney disease.
Many types of mutations in tumor suppressor p53 are oncogenic through gain-of-function. Therefore, targeting mutant p53 (mtp53) is a promising therapeutic approach to fight against many types of cancers. We report here a small molecule compound YK-3-237 that reduces acetylation
The Journal of pharmacology and experimental therapeutics, 354(2), 142-151 (2015-05-30)
Although activation of sirtuin-1 (SIRT1) has been shown to protect the kidney from acute injury, its role in renal fibrosis remains controversial since both inhibition and activation of SIRT1 have been reported to attenuate renal fibrosis. To resolve this conflict
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