Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

HDAC7:137 nM, HDAC9:70 nM, HDAC2:96 nM, HDAC4:56 nM, HDAC1:49 nM, HDAC8:140 nM, HDAC6:1008 nM, HDAC11:93 nM, HDAC3:43 nM, HDAC5:47 nM, HDAC10:40 nM, MBLAC2:<10 nM (EC50)

HDAC enzyme assay: All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software.

Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.(Only for Reference)

Ethanol: 26 mg/mL (72.53 mM), Sonication is recommended.

DMSO: 250 mg/mL (697.39 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.58 mM), Sonication is recommended.