| Chemical Properties | Back Directory | [InChI]
InChI=1S/C20H30N4O2.ClH/c1-4-7-8-19-21-17-15-16(10-12-20(25)22-26)9-11-18(17)24(19)14-13-23(5-2)6-3;/h9-12,15,26H,4-8,13-14H2,1-3H3,(H,22,25);1H/b12-10+; | [InChIKey]
RCLMPSZFYQJPQD-VHPXAQPISA-N | [SMILES]
C(N1C(=NC2=CC(/C=C/C(=O)NO)=CC=C12)CCCC)CN(CC)CC.Cl |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
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]. | [References]
[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 |
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