ZL0580 是ZL0590 的结构类似物，通过选择性的结合到 BD1 的 BRD4 结构域来诱导 HIV 的表观抑制。ZL0580通过抑制 Tat 转录激活和转录延长以及在 HIV 启动子上诱导抑制染色质结构来诱导 HIV 的抑制。
货号:ajcx16892
CAS:2377151-10-3
分子式:C25H23F3N4O4S
分子量：532.53
溶解度:DMSO: 250 mg/mL (469.46 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter[1][2][3].

[1]. Niu Q, et al. Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV. J Clin Invest. 2019 Jul 22;129(8):3361-3373. [2]. Vansant G, et al. Block-And-Lock Strategies to Cure HIV Infection. Viruses. 2020 Jan 10;12(1). pii: E84. [3]. Brasier AR, et al. Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling. Drug Discov Today. 2020 Jan;25(1):126-132.