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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-ZL0969
ZL0969

Chemical Structure : ZL0969

CAS No.: 3058109-33-1

ZL0969 (ZL-0969)

货号: PC-24899Not For Human Use, Lab Use Only.

ZL0969 is a potent, selective, and orally bioavailable BRD4 inhibitor with IC50 of 82 nM and 87 nM for BRD4 BD1 and BRD4 BD2, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZL0969 is a potent, selective, and orally bioavailable BRD4 inhibitor with IC50 of 82 nM and 87 nM for BRD4 BD1 and BRD4 BD2, respectively.
ZL0969 showed >10-fold binding selectivity for BRD4 BDs over other BET-family BDs, showed no detectable binding for the non-BET CBP BD.
ZL0969 displays a strong inhibitory activity on IL-6 (IC50=0.253 ± 0.034 µM), CIG5 (IC50 = 0.270 ± 0.023 µM), IL-8 (IC50 = 0.234 ± 0.032 µM), and ISG54 (IC50 = 0.242 ± 0.027 µM) gene expression in small airway epithelial cells (hSAECs).
ZL0969 disrupts epithelial mesenchymal transition (EMT).
ZL0969 (20 mg/kg) treatment via oral gavage reduced myofibroblast formation and deposition of denatured ECM (collagen and laminin a1) in the alveolar space and improved disease scores in in bleomycin-induced fibrosis mice model.
ZL0969 reduced a pathogenic population of alveolar progenitor cells expressing integrin (ITG)-A6/B4, tumor related protein 63 (Trp63) and keratin (Krt).

物理化学性质&存储条件

分子量 466.58
分子式 C27H34N2O5
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

2-(3,5-dimethyl-4-(3-(4-methylpiperazin-1-yl)propoxy)phenyl)-5,7-dimethoxy-4H-chromen-4-one

参考文献

1. Skibba M, et al. Respir Res. 2025 Jul 2;26(1):221.

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