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

Info

Catalogue Number 152433
Antigen/Gene or Protein Targets HDAC2/3
Type Inhibitor
Relevance 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.
On Target IC50 Potent and selective HDAC2/3 inhibitor (IC50 values are 16 and 30 nM, respectively)
Selectivity Exhibits >250-fold selectivity for HDAC2/3 over other HDAC isoforms.
Molecular Formula C24H21N3O2.HCl
lUPAC N-(2-Amino-phenyl)-4-(4-methylene-1-oxo-3,4-dihydro-1H-isoquinolin-2-ylmethyl)-benzamide.
Molecular Weight (g/mol) 419.91
In vitro applications 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, SNB-75 and U251.
When tested in culture against the acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1, MI-192 induced differentiation and was cytotoxic through promotion of apoptosis.
Solubility DMSO
Research Area Cancer, Epigenetics & Nuclear Signalling
Storage Ambient

References

There are 4 reference entries for this reagent.

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References: 4 entries

Boissinot et al. 2012. Leuk Res. 36(10):1304-10. PMID: 22818799.

Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192.

Europe PMC ID: 22818799

Gillespie et al. 2012. Arthritis Rheum. 64(2):418-22. PMID: 21952924.

Histone deacetylases are dysregulated in rheumatoid arthritis and a novel histone deacetylase 3-selective inhibitor reduces interleukin-6 production by peripheral blood mononuclear cells from rheumatoid arthritis patients.

Europe PMC ID: 21952924


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References: 4 entries

Boissinot et al. 2012. Leuk Res. 36(10):1304-10. PMID: 22818799.

Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192.

Gillespie et al. 2012. Arthritis Rheum. 64(2):418-22. PMID: 21952924.

Histone deacetylases are dysregulated in rheumatoid arthritis and a novel histone deacetylase 3-selective inhibitor reduces interleukin-6 production by peripheral blood mononuclear cells from rheumatoid arthritis patients.


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