MPT0G211 mesylate
Based on 1 publication(s) in Google Scholar
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.
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- CAS No.: 2151854-33-8
- Formula: C18H19N3O5S
- Molecular Weight:389.43
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Storage:
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Biological Activity
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HDAC6 0.291 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes[1]
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Dosage:50 mg/kg
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Administration:P.o.; daily for 3 months
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Result:Significantly ameliorated the spatial memory impairment.
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Animal Model:Female SCID mice (bearing MDA-MB-231 cells)[2]
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Dosage:25 mg/kg
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Administration:I.p.; qd; day 73 post-tumor injection
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Result:Significantly reduced numbers of nodules and lung weights.
Chemical Information
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CAS No. 2151854-33-8
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Molecular Weight 389.43
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Formula C18H19N3O5S
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SMILES
CS(=O)(O)=O.O=C(NO)C1=CC=C(CNC2=C3N=CC=CC3=CC=C2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[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. [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]
Calculators
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