A hydroxamate-based inhibitor of HDACs with an IC50 value of 30 nM; inhibits the growth of colon

LAQ824 – 5 mg

Brand:
Cayman
CAS:
404951-53-7
Storage:
-20
UN-No:
Non-Hazardous - /

LAQ824 is a hydroxamate-based inhibitor of histone deacetylases (HDACs) with an IC50 value of 30 nM.{26872,18374} It inhibits the growth of colon, breast, prostate, and non-small cell lung cancer cell lines at concentrations of less than 1 µM.{26872,18481} LAQ824 augments the actions of fludarabine (Item No. 14128) and imatinib mesylate (Item No. 13139) in human leukemia cells.{26871,26870} Through its effects on HDACs, LAQ824 induces acetylation of histones, α-tubulin, and heat shock protein 90 (Hsp90).{26870,16189} Acetylation of Hsp90 blocks its chaperone function, resulting in changes in levels of several client proteins, including estrogen receptor-α, Hsp72, and Raf-1.{16189,26868}  

 

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Description

A hydroxamate-based inhibitor of HDACs with an IC50 value of 30 nM; inhibits the growth of colon, breast, prostate, and non-small cell lung cancer cell lines at concentrations of less than 1 µM; augments the actions of fludarabine and imatinib mesylate in human leukemia cells

Formal name: (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide

Synonyms:  Dacinostat|NVP-LAQ824

Molecular weight: 379.5

CAS: 404951-53-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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