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Pracinostat Dihydrochloride is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 40-140 nM, used in cancer research. It also inhibits the activity of metallo-β-lactamase structural domain-containing protein 2 (MBLAC2) hydrolase with an EC50 of less than 10 nM.

Pracinostat dihydrochloride is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat dihydrochloride also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2) hydrolase activity with an EC50 below 10 nM[1][4].

[1] Novotny-Diermayr V, et al. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol Cancer Ther. 2010 Mar;9(3):642-52. DOI:10.1158/1535-7163.MCT-09-0689
[2] Wang H, et al. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720. DOI:10.1021/jm2003552
[3] Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood Cancer J. 2012 May;2(5):e69. DOI:10.1038/bcj.2012.14
[4] Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18(8):812-820. DOI:10.1038/s41589-022-01015-5