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ZL0420

CAS No. : 2230496-80-5

MCE 站：ZL0420

产品活性：ZL0420 是有效且选择性的 BET 溴结构域 4 (BRD4) 抑制剂，对 BRD4 BD1和 BRD4 BD2 的 IC₅₀ 分别为 27 nM 和 32 nM。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: ZL0420 is well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H₂O molecule. ZL0420 exhibits submicromolar potency of inhibiting the TLR3-dependent innate immune gene program, including ISG54, ISG56, IL-8, and Groβ genes in cultured human small airway epithelial cells (hSAECs) with IC₅₀s of 0.49-0.86 ?M.

In Vivo: ZL0420 demonstrates potent efficacy reducing airway inflammation in a mouse model with low toxicity. ZL0420 displays high efficacy and almost completely blocks the profound accumulation of neutrophils around the small and medium sized airways induced by poly(I:C) administration.

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