896683-78-6
896683-78-6 structure
- Name: STAMBP-IN-1
- Chemical Name: Acetamide, 2-[[3,4-dihydro-6-(4-morpholinyl)-4-oxo-3-(2-phenylethyl)-2-quinazolinyl]thio]-N-(2-furanylmethyl)-
- CAS Number: 896683-78-6
- Molecular Formula: C27H28N4O4S
- Molecular Weight: 504.6
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Deubiquitinase
- Create Date: 2022-10-31 15:20:47
- Modify Date: 2024-04-02 18:04:22
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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].
| Name | Acetamide, 2-[[3,4-dihydro-6-(4-morpholinyl)-4-oxo-3-(2-phenylethyl)-2-quinazolinyl]thio]-N-(2-furanylmethyl)- |
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| Description | 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]. |
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| Related Catalog | |
| In Vitro | 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). |
| Molecular Formula | C27H28N4O4S |
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| Molecular Weight | 504.6 |