产品
编 号:F578979
分子式:C27H28N4O4S
分子量:504.6
产品类型
结构图
CAS No: 896683-78-6
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产品详情
生物活性:
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM.
体外研究:
STAMBP-IN-1 (0.1-10 μM; 6 h) exhibits the most potent ability to selectively decrease NALP7 abundance as well as endogenous NALP7 abundance in THP-1 cells, but not NALP6.STAMBP-IN-1 (0.01-100 μM; 37 ℃; 2 h) inhibits cleavage of K63-linked di-Ub (200 nM) to mono-Ub by purified recombinant STAMBP (25 nM) in a concentration dependent manner.STAMBP-IN-1 (0.01-10 μM; 37 ℃; 60 min) blocks STAMBP mediated deubiquitination of Ub-NALP7 in vitro in a concentration-dependent manner.STAMBP-IN-1 exhibits toxicity against THP-1 cells with an IC50 of 106 μg/mL.