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MPT0G211

CAS No. : 2151853-97-1

MCE 站：MPT0G211

产品活性：MPT0G211 是一种高效、口服活性和选择性的 HDAC6 抑制剂 (IC₅₀=0.291?nM)。MPT0G211 对 HDAC6 的选择性是其他 HDAC 亚型的 1000 倍。MPT0G211 可以透过血脑屏障。MPT0G211 改善阿尔茨海默病模型中 tau 磷酸化和认知缺陷。MPT0G211 具有抗转移和神经保护作用。抗癌活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

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.
MPT0G211 inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins.
MPT0G211 significantly decreases the phosphorylation of tau by GSK3β inactivation.
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).
MPT0G211 inhibits MDA-MB-231 and MCF-7 cells growth (GI₅₀=16.19 and 5.6 μM, respectively).
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.

In Vivo: MPT0G211 (50?mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment.
MPT0G211 (25?mg/kg; i.p. ; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights.
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.

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