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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-ZL0580
ZL0580

Chemical Structure : ZL0580

CAS No.: 2377151-10-3

ZL0580 (ZL-0580)

货号: PC-73041Not For Human Use, Lab Use Only.

ZL0580 (ZL-0580) is a small molecule that induces epigenetic suppression of HIV via BRD4, suppresses PMA-induced HIV activation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ZL0580 (ZL-0580) is a small molecule that induces epigenetic suppression of HIV via BRD4, suppresses PMA-induced HIV activation.
ZL0580 induces epigenetic reprogramming of HIV LTR in J-Lat cells, suppresses HIV in in vitro HIV-infected human CD4+ T cells, did not significantly alter HIV DNA levels, but reduced HIV transcription in PBMCs.
ZL0580 suppresses HIV transcription ex vivo in PBMCs of viremic HIV-infected participants.
ZL0580 more selectively binds to the BRD4 BD1 domain (IC50=163 nM) instead of BD2 (IC50=1071 nM).
ZL0580 also displays approximately 6- to 11-fold selectivity for BRD4 over other BET proteins (IC50 ranged from approximately 0.9 to 1.9 μM) as well as over a non-BET BD protein, CBP (IC50 >10 uM).
ZL0580 inhibits Tat transactivation and key factors in HIV transcription elongation.

物理化学性质&存储条件

分子量 532.538
分子式 C25H23F3N4O4S
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

(S)-N-phenyl-1-((4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl)sulfonyl)pyrrolidine-2-carboxamide

参考文献

1. Niu Q, et al. J Clin Invest. 2019 Jul 22;129(8):3361-3373.

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