MPT0G211 mesylate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MPT0G211 mesylate 

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。

MPT0G211 mesylate

MPT0G211 mesylate Chemical Structure

CAS No. : 2151854-33-8

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MPT0G211 mesylate 的其他形式现货产品:

MPT0G211

生物活性

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].

IC50 & Target[1]

HDAC6

0.291 μM (IC50)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

分子量

389.43

Formula

C18H19N3O5S

CAS 号

2151854-33-8

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.

参考文献
  • [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.

    [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.

    [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.

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