1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. MPT0G211 mesylate

MPT0G211 mesylate 

Cat. No.: HY-123976A
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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.

For research use only. We do not sell to patients.

MPT0G211 mesylate Chemical Structure

MPT0G211 mesylate Chemical Structure

CAS No. : 2151854-33-8

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Description

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)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE 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.
Molecular Weight

389.43

Formula

C₁₈H₁₉N₃O₅S

CAS No.
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MPT0G211 mesylate
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HY-123976A
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