Thiomyristoyl

MCE 国际站：Thiomyristoyl

产品活性：Thiomyristoyl是高效特异性的SIRT2抑制剂，IC₅₀值为28 nM。

研究领域：Cell Cycle/DNA Damage | Epigenetics

In Vitro: Thiomyristoyl (TM) is a potent SIRT2-specific inhibitor with broad anticancer activity but little effect on non-cancerous cells. SIRT2-inhibition promotes c-Myc ubiquitination and degradation, suggesting the therapeutic potential of TM to target certain c-Myc-driven cancers. TM could inhibit SIRT2 with an IC₅₀ of 28 nM, but inhibits SIRT1 with an IC₅₀ value of 98 μM and does not inhibit SIRT3 even at 200 μM. TM inhibits three human breast cancer cell lines, MCF-7, MDA-MB-468, and MDA-MB-231.

In Vivo: TM inhibits tumor growth in mouse models of breast cancer. TM does not cause significant toxicity in mice and no significant weight loss is observed in TM-treated mice. S5H, the acetyl-a-tubulin level is moderately but statistically significantly increased in tumors from TM-treated mice compared with those from vehicle-treated mice, suggesting that TM indeed inhibits SIRT2 in vivo.

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