产品
编 号：F749393
分子式：C18H19N3O5S
分子量：389.43
分子式：C18H19N3O5S
分子量：389.43
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CAS No: 2151854-33-8
产品详情
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.
体内研究：
MPT0G211 mesylate (50?mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment.MPT0G211 mesylate (25?mg/kg; i.p.; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights.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.Animal Model:Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes
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)
Dosage:25?mg/kg
Administration:I.p.; qd; day 73 post-tumor injection
Result:Significantly reduced numbers of nodules and lung weights.
体外研究：
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.MPT0G211 mesylate inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins.MPT0G211 mesylate significantly decreases the phosphorylation of tau by GSK3β inactivation.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).MPT0G211 mesylate inhibits MDA-MB-231 and MCF-7 cells growth (GI50=16.19 and 5.6 μM, respectively).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.
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.
体内研究：
MPT0G211 mesylate (50?mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment.MPT0G211 mesylate (25?mg/kg; i.p.; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights.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.Animal Model:Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes
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)
Dosage:25?mg/kg
Administration:I.p.; qd; day 73 post-tumor injection
Result:Significantly reduced numbers of nodules and lung weights.
体外研究：
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.MPT0G211 mesylate inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins.MPT0G211 mesylate significantly decreases the phosphorylation of tau by GSK3β inactivation.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).MPT0G211 mesylate inhibits MDA-MB-231 and MCF-7 cells growth (GI50=16.19 and 5.6 μM, respectively).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.
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