STAMBP-IN-1

• CAT Number: I042654
• CAS Number: 896683-78-6
• Molecular Formula: C27H28N4O4S
• Molecular Weight: 504.60
• Purity: ≥95%
• Synonyms: N-(furan-2-ylmethyl)-2-[6-morpholin-4-yl-4-oxo-3-(2-phenylethyl)quinazolin-2-yl]sulfanylacetamide
• InChI: InChI=1S/C27H28N4O4S/c32-25(28-18-22-7-4-14-35-22)19-36-27-29-24-9-8-21(30-12-15-34-16-13-30)17-23(24)26(33)31(27)11-10-20-5-2-1-3-6-20/h1-9,14,17H,10-13,15-16,18-19H2,(H,28,32)
• InChIKey: HBAWGWWMULJGHR-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=CC3=C(C=C2)N=C(N(C3=O)CCC4=CC=CC=C4)SCC(=O)NCC5=CC=CO5

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].

Reference

[1]. Bednash JS,et al. Targeting the deubiquitinase STAMBP inhibits NALP7 inflammasome activity. Nat Commun. 2017 May 11;8:15203.
 [Content Brief]