產(chǎn)品目錄

規(guī)格	5 mg 10 mg 25 mg 50 mg 100 mg
CAS	2151853-97-1
別名	N/A
化學(xué)名	N/A
分子式	C17H15N3O2
分子量	293.32
溶解度	N/A
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities[1][2][3].

MPT0G211 (0.1 μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibits the phosphorylation of tau Ser396[1].MPT0G211 inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins[1].MPT0G211 significantly decreases the phosphorylation of tau by GSK3β inactivation[1].MPT0G211 (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 inhibits MDA-MB-231 and MCF-7 cells growth (GI50=16.19 and 5.6 μM, respectively)[2].In AML cells, MPT0G211 potentiated the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis[3].

MPT0G211 (50 mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment[1].MPT0G211 (25?mg/kg; i.p. ; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights[2].MPT0G211 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].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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