MI-192 HCl

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Research Areas >> Neurological Disease

Signaling Pathways >> Epigenetics >> HDAC

MI-192 (0.15-1 μM; 72 h) induces differentiation and is cytotoxic through promotion of apoptosis in acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1[1]. Apoptosis Analysis[1] Cell Line: HL60 and Kasumi-1 cells Concentration: 150 nM, 300 nM, 500 nM, 1 μM Incubation Time: 72 h Result: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells.

MI-192 (40 mg/kg; i.p; once a day; for 3 days) shows the neuroprotective activity in the mouse brain subjected to photothrombotic stroke[2]. Animal Model: Adult male outbred mice CD-1 (20-25 g) with photothrombotic stroke (PTS)[2] Dosage: 40 mg/kg Administration: i.p; once a day; for 3 days Result: Reduced the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, decreased the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere.

[1]. Marjorie Boissinot, et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leuk Res. 2012 Oct;36(10):1304-10.

[2]. S V Demyanenko, et al. The Neuroprotective Effect of the HDAC2/3 Inhibitor MI192 on the Penumbra After Photothrombotic Stroke in the Mouse Brain. Mol Neurobiol. 2020 Jan;57(1):239-248.