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MPT0G211

Catalog No. T60616 CAS 2151853-97-1

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

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MPT0G211, CAS 2151853-97-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 728.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,390.00
500 mg	In stock	$ 2,780.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 99.91%

Purity: 99.07%

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Description	MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.
Targets&IC50	HDAC6:0.291 μM
In vitro	MPT0G211 (0.1 μM; cells transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibits the phosphorylation of tau Ser396[3]. MPT0G211 inhibits HDAC6/Hsp90 binding, leading to subsequent proteasomal degradation of polyubiquitinated proteins[3]. MPT0G211 significantly decreases the phosphorylation of tau through GSK3β inactivation[3]. MPT0G211 (0.1 μM; 24 hours) significantly attenuates the phosphorylation of tau at Ser396 and Ser404 in both cell lines (SH-SY5Y and Neuro-2a cells transfected for 24 h with pCAX APP 695 and pRK5-EGFP-Tau P301L)[3]. MPT0G211 inhibits the growth of MDA-MB-231 and MCF-7 cells (GI50=16.19 and 5.6 μM, respectively)[2].In AML cells, MPT0G211 potentiates the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis[1].
In vivo	MPT0G211 (50 mg/kg; oral administration; daily for 3 months) significantly ameliorates spatial memory impairment[3]. MPT0G211 (25 mg/kg; intraperitoneal injection; once daily; day 73 post-tumor injection) reduces the numbers of nodules and lung weights[2]. MPT0G211 treatment not only diminishes tau phosphorylation by inhibiting GSK3β activity but also enhances the acetylation of Hsp90. This leads to the downregulation of HDAC6/Hsp90 binding and facilitates proteasomal degradation of polyubiquitinated phosphorylated tau[3].

Molecular Weight	293.32
Formula	C17H15N3O2
CAS No.	2151853-97-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (306.83 mM), Sonication is recommended.

References and Literature

1. 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. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max

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Keywords

MPT0G211 2151853-97-1 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibitor inhibit

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