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Chemical Structure : I-BET282
CAS No.: 1422554-34-4
Catalog No.: PC-20162Not For Human Use, Lab Use Only.
I-BET282 is a potent and selective pan-inhibitor of bromodomain and extra terminal (BET) proteins with pIC50 of 7.4 for BRD4-BD1, ITC Kd of 47.5 nM for BRD4, shows equivalent potency against BD1 and BD2 domains.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $378 | In stock | |
| 100 mg | Get quote |
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I-BET282 is a potent and selective pan-inhibitor of bromodomain and extra terminal (BET) proteins with pIC50 of 7.4 for BRD4-BD1, ITC Kd of 47.5 nM for BRD4, shows equivalent potency against BD1 and BD2 domains.
I-BET282 is a pan-inhibitor of all eight BET bromodomains (BRD2, BRD3, BRD4, and BRDT, each one contains two bromodomains (BD1 and BD2), and selectivity over other representative bromodomain-containing proteins.
I-BET282 binds to the bromodomain of CBP with an affinity constant of 1.73 uM by ITC assays, 36-fold window versus BRD4.
I-BET282 shows cellular potency with pIC50 of 7.0 and 6.5 in the human whole blood assays and in the IL-6 assays, respectively.
I-BET282 showed a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or3A4.
I-BET282E (I-BET282 mesylate) (3 mg/kg, p.o.) shows in vivo efficacy in the rat collagen-induced arthritis (CIA) model.
| M.Wt | 450.54 | |
| Formula | C25H30N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-4-(8-methoxy-1-(1-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole |
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1. Katherine L Jones, et al. J Med Chem. 2021 Aug 26;64(16):12200-12227.
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