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Hsp70-Bim PPI inhibitor JL-15

Chemical Structure : Hsp70-Bim PPI inhibitor JL-15

CAS No.:

Hsp70-Bim PPI inhibitor JL-15 (Hsp70-Bim inhibitor)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 476.02
Formula C28H30ClN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

4'-(4-Chloro-3,5-dimethylphenoxy)-3-hydroxy-5-((2-(piperidin-1-yl)ethyl)amino)-[1,1'-biphenyl]-4-carbonitrile

References

1. Maojun Jiang, et al. J Med Chem. 2024 Jul 16. doi: 10.1021/acs.jmedchem.4c00780.

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