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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-I-BET282
I-BET282

Chemical Structure : I-BET282

CAS No.: 1422554-34-4

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I-BET282 (I-BET 282)

货号: 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.

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10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3780 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 450.54
分子式 C25H30N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

1. Katherine L Jones, et al. J Med Chem. 2021 Aug 26;64(16):12200-12227.

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