Dacinostat

  • Chemical Properties
CAS No. 404951-53-7 Cat. No. BCP01747
Name Dacinostat
Synonyms LAQ824;LAQ-824;NVP-LAQ824;LA Q824;NVP LAQ824;NVPLAQ824;
Formula C22H25N3O3 M. Wt 379.45
  • Biological Activity
Description LAQ824 activates the expression of the gene encoding the p21 cell cycle inhibitor by activating the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM. LAQ824 inhibits the cell growth of both H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively, and the antiproliferative effect of LAQ824 is selective toward the tumor cell lines while inducing only growth arrest in normal fibroblasts. Furthermore, LAQ824 induces a dose-dependent increase of p21 protein in A549 cells and an increase in the hypophosphorylated state of the Rb tumor suppressor.A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages.
Pathways Cell Cycle/DNA Damage Epigenetics 
Targets HDAC 

Structure

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