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Contributor Information

  • Name Ron Grigg
  • Institute University of Leeds

Tool Details

  • Tool name: HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)
  • Molecular formula: C24H21N3O2.HCl
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: 419.91
  • 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, 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.
  • 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.
  • Research area: Apoptosis and Programmed Cell Death; Cancer; Plant Science
  • Selectivity: Exhibits >250-fold selectivity for HDAC2/3 over other HDAC isoforms.
  • IUPAC: N-(2-Amino-phenyl)-4-(4-methylene-1-oxo-3,4-dihydro-1H-isoquinolin-2-ylmethyl)-benzamide.
  • IC50: Potent and selective HDAC2/3 inhibitor (IC50 values are 16 and 30 nM, respectively)

  • For Research Use Only

Target Details

  • Target molecular weight: 419.91
  • Primary target: HDAC2/3

Application Details

  • 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, 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.

Handling

  • Purity: 419.91 g/mol
  • Solubility: DMSO
  • Storage conditions: Ambient
  • Shipping conditions: Dry Ice

Documentation

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References

  • •  WO2013005049 PMID: 22818799