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[1].
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[1].
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[1].
STAMBP-IN-1 (0.01-10 μM; 37 ℃; 60 min) blocks STAMBP mediated deubiquitination of Ub-NALP7 in vitro in a concentration-dependent manner[1].
STAMBP-IN-1 exhibits toxicity against THP-1 cells with an IC50 of 106 μg/mL[1].
Western Blot Analysis[1]
| 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). |
[1]. Bednash JS,et al. Targeting the deubiquitinase STAMBP inhibits NALP7 inflammasome activity. Nat Commun. 2017 May 11;8:15203.