MPT0G211 mesylate
Based on 1 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2151854-33-8
- 화학식: C18H19N3O5S
- 분자량:389.43
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MPT0G211 mesylate
More
Biological Activity
제품 설명
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (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.
Chemical Information
-
CAS No. 2151854-33-8
-
분자량 389.43
-
화학식 C18H19N3O5S
-
SMILES
CS(=O)(O)=O.O=C(NO)C1=CC=C(CNC2=C3N=CC=CC3=CC=C2)C=C1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
순도&문서
References
[1]. Fan SJ, 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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MPT0G211 mesylate Related Classifications
HY-123976A Related Classifications
Powered by Bioz