STAMBP-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BC-1471 是一种新型选择性去泛素酶 STAM 结合蛋白 (STAMBP) 拮抗剂，可降低 NALP7 蛋白水平并抑制 TLR 激动后 IL-1β 的释放。BC-1471 是 STAMBP 去泛素酶活性的小分子抑制剂，可降低 NALP7 蛋白水平并抑制 TLR 激动后 IL-1β 的释放。

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

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 deubi quitination 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. Western Blot Analysis Cell Line:THP-1 cells Concentration:0.01, 0.1, 1, 10, and 100 μM Incubation Time:6 hours Result:Inhibited the activity of STAMBP to cleave recombinant di-Ub in a concentrationdependent manner with an IC50 of 0.33 mM (0.09-1.21 mM).

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Others

Other Targets

deubiquitinase STAM-binding protein (STAMBP)

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896683-78-6

504.6

C27H28N4O4S

>98% (HPLC)

In Vitro:?DMSO : 3.29 mg/mL (6.52 mMw)

O=C(NCC1=CC=CO1)CSC(N2CCC3=CC=CC=C3)=NC4=C(C=C(N5CCOCC5)C=C4)C2=O

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(-20℃)

With Ice Pack

≥ 2 years