MPT0G211 mesylate 是一种高效、口服活性和选择性的HDAC6抑制剂 (IC50=0.291 nM)。MPT0G211 mesylate 对 HDAC6 的选择性是其他 HDAC 亚型的 1000倍。MPT0G211 mesylate 可以透过血脑屏障。MPT0G211 mesylate 改善阿尔茨海默病模型中 tau 磷酸化和认知缺陷。MPT0G211 mesylate 具有抗转移和神经保护作用。抗癌活性。
| 生物活性 | MPT0G211 mesylate is a potent, orally active and selectiveHDAC6inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective forHDAC6over otherHDACisoforms. 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]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | MPT0G211 mesylate (0.1 μM; Cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibited the phosphorylation of tau Ser396[1].
MPT0G211 mesylate inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins[1].
MPT0G211 mesylate significantly decreases the phosphorylation of tau by GSK3β inactivation[1].
MPT0G211 mesylate (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 mesylate inhibits MDA-MB-231 and MCF-7 cells growth (GI50=16.19 and 5.6 μM, respectively)[2].
In AML cells, MPT0G211 mesylate potentiates the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis[3].
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体内研究
(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 APPSweand tauP301Lmutant transgenes[1] | | Dosage: | 50 mg/kg | | Administration: | P.o.; daily for 3 months | | Result: | Significantly ameliorated the spatial memory impairment. |
| 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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