Thiomyristoyl is an inhibitor of Sirt2 and Sirt1 with IC50 of 28 nM, 98 μM.
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Thiomyristoyl is an effective and specific inhibitor of SIRT2, exhibiting broad anti-cancer activity with minimal effects on non-cancerous cells. The inhibition of SIRT2 by Thiomyristoyl promotes ubiquitination and degradation of c-Myc, indicating potential therapeutic value against certain c-Myc-driven cancers. Thiomyristoyl inhibits SIRT2 with an IC50 of 28 nM, while it inhibits SIRT1 with an IC50 of 98 μM, and does not inhibit SIRT3 even at 200 μM. Thiomyristoyl has been shown to inhibit three human breast cancer cell lines: MCF-7, MDA-MB-468, and MDA-MB-231[1].
Thiomyristoyl 动物研究
Animal study
In a mouse model of breast cancer, Thiomyristoyl significantly suppresses tumor growth without apparent toxicity to the mice, as no significant weight loss was observed in mice treated with TM. Compared to control-treated mice, Thiomyristoyl-treated mice showed a moderate but statistically significant increase in acetylated-α-tubulin levels in tumors, confirming the in vivo inhibition of SIRT2 by Thiomyristoyl[1].
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