Pracinostat dihydrochloride

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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.

For research use only. We do not sell to patients.

Pracinostat dihydrochloride Chemical Structure

CAS No. : 929016-98-8

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Other In-stock Forms of Pracinostat dihydrochloride:

Pracinostat

Other Forms of Pracinostat dihydrochloride:

Pracinostat In-stock

7 Publications Citing Use of MCE Pracinostat dihydrochloride

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•Related Small Molecules:

•Related Proteins:

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Metallo-β-lactamase

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 40 nM (HDAC10), 43 nM (HDAC3), 47 nM (HDAC5), 49 nM (HDAC1), 56 nM (HDAC4), 70 nM (HDAC9), 93 nM (HDAC11), 96 nM (HDAC2), 137 nM (HDAC7), 140 nM (HDAC8), 1008 nM (HDAC6)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.48 μM Compound: 3, SB939	Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
COLO 205	IC₅₀	0.56 μM Compound: 3, SB939	Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	IC₅₀	0.48 μM Compound: 3, SB939	Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
PC-3	IC₅₀	0.34 μM Compound: 3, SB939	Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]

Molecular Weight

431.40

Formula

C₂₀H₃₂Cl₂N₄O₂

CAS No.

929016-98-8

SMILES

CCN(CCN1C2=CC=C(C=C2N=C1CCCC)/C=C/C(NO)=O)CC.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]