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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-SKLB-39b
SKLB-39b

Chemical Structure : SKLB-39b

CAS No.: 3051945-94-6

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SKLB-39b (SKLB39b)

货号: PC-28446Not For Human Use, Lab Use Only.

SKLB-39b is a potent, selective BET bromodomain 1 (BD1) inhibitor with IC50 of 42 nM for BRD4-BD1, with >100-fold BD2 selectivity, disrupts BRD4-BD1-p62 interaction and exhits antifibrotic effect.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SKLB-39b is a potent, selective BET bromodomain 1 (BD1) inhibitor with IC50 of 42 nM for BRD4-BD1, with >100-fold BD2 selectivity, disrupts BRD4-BD1-p62 interaction and exhits antifibrotic effect.
inhibits fibroblast activation by inducing protective autophagy against NIH3T3cells with IC50 of 2.5 uM.
SKLB-39b markedly reduced α-SMA expression and its colocalization with BRD4 in activated fibroblasts.
SKLB-39b restores ULK1-dependent autophagy, inhibits TGF-β1-induced A549 cell migration more effectively than JQ1.
SKLB-39b exerts anti-fibrotic effects via reactivation of protective autophagy, promotes autophagosome-lysosome fusion and induces complete autophagic flux.
SKLB-39b shows selective binding BRD4-BD1 with BLI KD of 208 nM.
SKLB-39b (30 or 60 mg/kg, i.p.) improved survival in bleomycin-induced pulmonary fibrosis in mice model of bleomycin-induced pulmonary fibrosis.
SKLB-39b engages BRD4-BD1 through Leu92 and Ile146, weakens BRD4-BD1-p62 association, reduces p62 protein accumulation, and restores protective autophagy in activated fibroblasts.

物理化学性质&存储条件

分子量 385.85
分子式 C20H20ClN3O3
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

1-(3-chloro-4-((2-methyl-3-oxocyclopent-1-en-1-yl)amino)phenyl)-3-(4-methoxyphenyl)urea

参考文献

1. Zhang J, et al. Cell Chem Biol. 2026 Oct 8:S2451-9456(26)00335-1.

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