Purinostat mesylate is a potent, highly selective class I and IIb HDAC inhibitor with IC50 of 0.81, 1.4, 1.7, and 3.8 nM for class I HDAC1, 2, 3, and 8, and 11.5, 1.1 nM for class IIb HDAC 6 and 10, respectively.
Purinostat mesylate displays much weaker activity against HDAC IIa and IV (HDAC4,5,7,9 11) with IC50 of 426-3,349 nM, also has no significant inhibitory activity on 89 kinase enzymes involved in tumor regulation.
Purinostat mesylate showed approximately 100-fold higher than Chidamide (Tucidinostat, Cat. PC-35344) inhibition on HDAC1, 2, 8, and 10 subtypes.
Purinostat mesylate showed better inhibitory effects than LBH589 (Panobinostat, Cat. PC-42468) against various hematologic tumor cell lines with IC50 values at nanomolar or subnanomolar.
Purinostat mesylate effectively increased the levels of Ac-H3, Ac-H4, and decreased HSP90 in a concentration-dependent manner in vitro of Ph+ leukemia cell lines, consistent with the BCR-ABL downregulation, p-SRC and STAT5 were also significantly suppressed.
Purinostat mesylate (5 mg/kg) exerted the robust antitumor activity on BL-2 secondary transplantation mouse model of Ph+ B-ALL.
Purinostat mesylate showed potent antileukemia effects in BCR-ABL(T315I)–induced primary B-ALL mice.