MedChemExpress - Model MPT0G211 -2151853-97-1
MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities[1][2][3].MCE products for research use only. We do not sell to patients.
MPT0G211
MCE China：MPT0G211
Brand：MedChemExpress (MCE)
Cat. No.HY-123976
CAS：2151853-97-1
Purity：99.79%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities.
In Vitro：MPT0G211 (0.1?μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24?h) significantly inhibits the phosphorylation of tau Ser396[1]. MPT0G211 inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins[1]. MPT0G211 significantly decreases the phosphorylation of tau by GSK3β inactivation[1]. MPT0G211 (0.1?μM; 24 hours) significantly attenuates the phosphorylation of tau Ser396 and Ser404 in both cell lines (SH-SY5Y and Neuro-2a cells were transfected for 24?h with pCAX APP 695 and pRK5-EGFP-Tau P301L)[1]. MPT0G211 inhibits MDA-MB-231 and MCF-7 cells growth (GI50=16.19 and 5.6 μM, respectively)[2]. In AML cells, MPT0G211 potentiated the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis[3].
In Vivo：MPT0G211 (50?mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment[1]. MPT0G211 (25?mg/kg; i.p. ; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights[2]. MPT0G211 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].
IC50 & Target：HDAC6 0.291 μM (IC50)
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References：
[1]. Fan SJ, Huang FI, 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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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