LAQ824 (also known as NVP-LAQ824 or Dacinostat), a derivative of 4-aminomethylcinnamic hydroxamic acid, is a novel and potent inhibitor of histone deacetylase (HDAC) that inhibits the activity of HDAC with 50% inhibition concentration IC50 value of 0.03 μM. LAQ824 has been found to inhibit the growth of a variety of cancer cell lines, including colon cancer H1299 and HCT116 cells, breast cancer MDA435 cells, prostate cancer DU145 and PC3 cells and non-small cell lung cancer A549 cells, with IC50 value < 1 μM and induce apoptosis in human breast cancer SKBR-3, BT-474 and MB-468 cells. LAQ824 also dose- and time-dependently inhibits the growth of multiple myeloma cells.
insoluble in H2O; insoluble in EtOH; ≥17.45 mg/mL in DMSO
CAS Registry #
404951-53-7
Background
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.
References
Catley L, et al. Blood. 2003 Oct 1;102(7):2615-22.
Storage/Stability
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.