HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)
Invented at University of Leeds
- Datasheet
- References (4)
- Inventor Info
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: 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
Add a reference
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.
Add a reference
