HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)

MI-192 be a potential therapeutic agent for use in leukaemia and HDAC-selective inhibition may improve the therapeutic margin of safety.

Contributors

Inventor Institute
Ron Grigg University of Leeds
Cat. #: 152433
Tool sub type: Inhibitor
Research Fields: Apoptosis and autophagy
Application: Promotes apoptosis of leukemia cell lines in vitro. Also attenuates IL-6 production in rheumatoid arthritis PBMCs in vitro. MI-192 (CRT0163458) shows potent activity in a number of cell lines tested using the NCI-60 cell panel. MI-192 was tested using the following NCI-60 cell lines: Leukemia cell lines: CCRF-CEM, HL-60 (TB), K-562, MOLT-4 and RPMI-8226. Colon Cancer cell lines: COLO205, HCC-2998, HCT-116, HCT-15, HT29, KM12 and SW-620. CNS Cancer cell lines: SF-268, SF-295, SF-539, SNB-19, …
Purpose: Inhibitor
Product description: MI-192 is a novel benzamide-based compound with marked selectivity for the class I enzymes, HDAC2 (histone-deacetylase 2) and HDAC3 (histone-deacetylase 3). MI-192 is also a histone-deacetylase (HDAC)-3 selective inhibitor. MI-192 might have potential in the treatment of rheumatoid arthritis, and HDAC-selective inhibition may improve the therapeutic margin of safety. Studies in various cancer cell lines have also revealed that MI-192 might be a potential therapeutic agent for use in leukaemia.
Molecular weight: 419.91
Selectivity: Exhibits >250-fold selectivity for HDAC2/3 over other HDAC isoforms.
Primary target: HDAC2/3
Storage conditions: Ambient
Shipping conditions: Dry Ice
Solubility: DMSO
References:

WO2013005049 PMID: 22818799

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