名称 | ZL0420 |
描述 | ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with nanomolar binding affinities to the bromodomains (BDs) of BRD4, exhibiting IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. |
体外活性 | ZL0420 effectively binds to the acetyl-lysine (KAc) binding pocket of BRD4, establishing essential interactions, notably critical hydrogen bonds directly with Asn140 and indirectly with Tyr97 through a water molecule. It demonstrates submicromolar efficacy in suppressing the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs), with IC50 values ranging from 0.49 to 0.86 μM [1]. |
体内活性 | ZL0420 demonstrates potent efficacy in reducing airway inflammation with low toxicity in a mouse model, almost completely blocking the significant accumulation of neutrophils around small and medium-sized airways induced by poly(I:C) administration [1]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 59 mg/mL (199.11 mM)
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关键字 | ZL 0420 | inhibit | Epigenetic Reader Domain | (E/Z)-ZL0420 | BRD4 | ZL0420 | airway inflammation | immune response genes | ZL-0420 | BET | bromodomains | Inhibitor |
相关产品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
相关库 | 组蛋白修饰化合物库 | 经典已知活性库 | 表观遗传库 | 激酶抑制剂库 | 抑制剂库 | PPI抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 |