Droxinostat

99873-43-5

C11H14ClNO3

DMSO : >= 150 mg/mL (615.54 mM)

Epigenetics; Cell Cycle/DNA Damage

Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 uM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10. IC50 Value: 16.9 uM(HDAC3); 2.47 uM(HDAC6); 1.46 uM(HDAC8) Target: HDAC3/6/8 in vitro: Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 uM, 2.47 uM, and 1.46 uM, respectively, without inhibiting other HDAC members (IC50 > 20 uM). In MCF-7 breast cancer cells, Droxinostat (10 uM�100 uM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis. in vivo: In SCID mice models, Droxinostat (30 uM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.