Chemical Structure : Hsp70-Bim PPI inhibitor JL-15
CAS No.:
Hsp70-Bim PPI inhibitor JL-15
(Hsp70-Bim inhibitor)
货号: PC-22674Not For Human Use, Lab Use Only.
Hsp70-Bim PPI inhibitor JL-15 is a potent, specific Hsp70-Bim protein-protein interaction (PPI) inhibitor with Kd of 123 nM, inhibits CML cells in the sub-μM range, overcomes BCR-ABL-independent tyrosine kinase inhibitor resistance.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
Hsp70-Bim PPI inhibitor JL-15 is a potent, specific Hsp70-Bim protein-protein interaction (PPI) inhibitor with Kd of 123 nM, inhibits CML cells in the sub-μM range, overcomes BCR-ABL-independent tyrosine kinase inhibitor resistance.
JL-15 potently induced apoptosis in K562, BV173, and K562-R3 with EC50 values in the sub-μM range, while no obvious toxicity was found in HEK293 and BaF3 even at a relatively higher concentration.
exhibited the same selective killing activity against TKI-sensitive and TKI-resistant CML cells.
JL-15 dose-dependently disrupted the Hsp70-Bim complex and showed no obvious influence on the Hsp70-Bag3 complex.
JL-15 significantly decreased the expression levels of AKT, Raf-1, and eIF4E in K562 cells, induces apoptosis.
物理化学性质&存储条件
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分子量
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476.02
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分子式
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C28H30ClN3O2
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4'-(4-Chloro-3,5-dimethylphenoxy)-3-hydroxy-5-((2-(piperidin-1-yl)ethyl)amino)-[1,1'-biphenyl]-4-carbonitrile
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参考文献
1. Maojun Jiang, et al. J Med Chem. 2024 Jul 16. doi: 10.1021/acs.jmedchem.4c00780.
