| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:MPT0G211
CAS:2151853-97-1
Purity:详情请见官网 Package:50 mg;10 mg;5 mg;2 mg;100 mg;1 mL;25 mg;
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| Company Name: |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
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| Tel: |
021-59167510 18117107507 |
| Email: |
vip@med-life.cn |
| Products Intro: |
Product Name:MPT0G211
CAS:2151853-97-1
Purity:>=99% Package:25mg;100mg;10mg;5mg;50mg;200mg;500mg;10mM*1mLinDMSO
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| Company Name: |
RD International Technology Co., Limited
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| Tel: |
18024082417 |
| Email: |
market@ubiochem.com |
| Products Intro: |
Product Name:MPT0G211
CAS:2151853-97-1
Purity:5mg;10mg;50mg;100mg;250mg;500mg;1g Package:5mg;10mg;50mg;100mg;250mg;500mg;1g
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| | Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Basic information |
| | Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Chemical Properties |
| density | 1.343±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | form | Solid | | pka | 8.90±0.10(Predicted) | | color | Light yellow to khaki |
| | Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Usage And Synthesis |
| Biological Activity | 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 (25mg/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]. | | References | [1]. Fan SJ, Huang FI, 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. |
| | Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Preparation Products And Raw materials |
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