Pracinostat

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

Product Specifications

CAS Number

[929016-96-6]

Product Name Alternative

SB939

UNSPSC

12352005

Hazard Statement

H228, H315, H319

Target

Apoptosis; Beta-lactamase; HDAC

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pracinostat.html

Purity

99.80

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

ONC(/C=C/C1=CC=C2N(C(CCCC)=NC2=C1)CCN(CC)CC)=O

Molecular Formula

C20H30N4O2

Molecular Weight

358.48

Precautions

H228, H315, H319

References & Citations

[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.|[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.|[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.|[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.