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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 Chemical Structure
CAS No. : 2151854-33-8
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是否有货 |
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100 mg |
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询价 |
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250 mg |
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500 mg |
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* Please select Quantity before adding items.
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].
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IC50 & Target[1] |
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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.
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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].
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. |
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Formula |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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[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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