Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]-
- CAS No.
- 2151853-97-1
- Chemical Name:
- Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]-
- Synonyms
- Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]-
- CBNumber:
- CB85568949
- Molecular Formula:
- C17H15N3O2
- Molecular Weight:
- 293.32
- MDL Number:
- MFCD32063565
- MOL File:
- 2151853-97-1.mol
Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
Benzamide, N-hydroxy-4-[(8-quinolinylamino)methyl]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 23963 | 58 |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 5012 | 58 |
RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9274 | 58 |
Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12007 | 58 |