Drug intelligence / Profile preview

thiomyristoyl

Development stage
Preclinical
Lead developer
Cornell University
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Thiomyristoyl is a potent, cell-permeable, and selective small molecule inhibitor of **Sirtuin 2 (SIRT2)**. Originally identified for its extensive anticancer activity, it works by inhibiting SIRT2-mediated deacetylation and demyristoylation of various protein substrates. Beyond oncology, thiomyristoyl has demonstrated significant anti-inflammatory properties in preclinical models. Specifically, it has been shown to ameliorate experimental colitis by blocking the differentiation of **Th17 cells**, a process mediated through the inhibition of the **STAT3/IL-6** signaling pathway. By modulating the acetylation status of key immune regulators, thiomyristoyl represents a potential therapeutic candidate for inflammatory bowel diseases (IBD), including Crohn's disease and ulcerative colitis.

Other names
thiomyristoyl-lysineN6-(1-thiotetradecanoyl)-L-lysine
02

Targets

SIRT2 (NAD-dependent protein deacetylase sirtuin-2)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)

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