JNJ 26481585 dihydrochloride - Quisinostat dihydrochloride

Based on 92 publications in PubMed 9 10 92

Axon 2529

CAS [875320-31-3]

MF C21H26N6O2.2HCl
MW 467.39

Purity: 99%
Soluble in DMSO

JNJ 26481585 dihydrochloride

Description

Potent, orally available second-generation pan-HDAC inhibitor (highest IC50 value 0.11 nM for HDAC1, and sub-nanomolar for HDAC2, HDAC4, HDAC10, and HDAC11 in vitro) with activity in human leukemia. JNJ-26481585 induces continuous acetylation of histone H3, activation of the caspase cascade, and upregulation of p21, resulting in apoptosis and cell cycle arrest in the myeloma cells at low nanomolar concentrations. JNJ26481585 also potently induced tubulin acetylation.

S. Deleu et al. The effects of JNJ-26481585, a novel hydroxamate-based histone deacetylase inhibitor, on the development of multiple myeloma in the 5T2MM and 5T33MM murine models. Leukemia. 2009 Oct;23(10):1894-903.

J. Arts et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.

Apoptosis Cell Cycle Regulation Cell Signaling & Oncology Epigenetics DNA-damage Response EC 3.5.1.98 HDAC

Potent, orally available second-generation pan-HDAC inhibitor

Chemical name

N-hydroxy-2-(4-(((1-methyl-1H-indol-3-yl)methylamino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide dihydrochloride

Parent CAS No.

[875320-29-9]

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