| Identification | Back Directory | [Name]
Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]-, compd. with methanesulfonate (1:1) | [CAS]
2151854-33-8 | [Synonyms]
MPT0G211 mesylate
Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]-, compd. with methanesulfonate (1:1) | [Molecular Formula]
C18H19N3O5S | [MOL File]
2151854-33-8.mol | [Molecular Weight]
389.43 |
| Hazard Information | Back Directory | [Uses]
MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities[1][2][3]. | [in vivo]
MPT0G211 mesylate (50 mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment[1].
MPT0G211 mesylate (25 mg/kg; i.p.; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights[2].
MPT0G211 mesylate treatment not only diminishes tau phosphorylation by inhibition GSK3β activity but also enhances the acetylation of Hsp90, which causes the downregulation of HDAC6/Hsp90 binding and facilitates proteasomal degradation of polyubiquitinated p-tau[1]. | Animal Model: | Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes[1] | | Dosage: | 50?mg/kg | | Administration: | P.o.; daily for 3 months | | Result: | Significantly ameliorated the spatial memory impairment.
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| Animal Model: | Female SCID mice (bearing MDA-MB-231 cells)[2] | | Dosage: | 25?mg/kg | | Administration: | I.p.; qd; day 73 post-tumor injection | | Result: | Significantly reduced numbers of nodules and lung weights.
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| [IC 50]
HDAC6: 0.291 μM (IC50) | [References]
[1] Fan SJ, et al. The novel histone de acetylase 6 inhibitor, MPT0G211, ameliorates tau phosphorylation and cognitive deficits in an Alzheimer's disease model. Cell Death Dis. 2018;9(6):655. Published 2018 May 29. DOI:10.1038/s41419-018-0688-5
[2] Hsieh YL, et al. Anti-metastatic activity of MPT0G211, a novel HDAC6 inhibitor, in human breast cancer cells in vitro and in vivo. Biochim Biophys Acta Mol Cell Res. 2019;1866(6):992-1003. DOI:10.1016/j.bbamcr.2019.03.003
[3] Tu HJ, et al. The anticancer effects of MPT0G211, a novel HDAC6 inhibitor, combined with chemotherapeutic agents in human acute leukemia cells. Clin Epigenetics. 2018;10(1):162. Published 2018 Dec 29. DOI:10.1016/j.bbamcr.2019.03.003 |
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