MPT0G211
Based on 1 publication(s) in Google Scholar
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.
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- Pureza: 99.79%
- No. CAS: 2151853-97-1
- Fòrmula: C17H15N3O2
- Peso molecular:293.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MPT0G211
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Actividad biológica
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HDAC6 0.291 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
5.33 μM
Compound: MPTOG211
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Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
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[PMID: 34052677] |
| NCI-H929 | GI50 |
9.14 μM
Compound: 13
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Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay
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[PMID: 29304284] |
| PC-3 | IC50 |
3.28 μM
Compound: MPTOG211
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Antiproliferative activity against human PC-3 cells
Antiproliferative activity against human PC-3 cells
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[PMID: 34052677] |
| RPMI-8226 | GI50 |
7.49 μM
Compound: 13
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Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay
Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay
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[PMID: 29304284] |
| U-266 | GI50 |
40.61 μM
Compound: 13
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Antiproliferative activity against human U266 cells after 48 hrs by SRB assay
Antiproliferative activity against human U266 cells after 48 hrs by SRB assay
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[PMID: 29304284] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes[1]
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Dosage:50 mg/kg
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Administration:P.o.; daily for 3 months
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Result:Significantly ameliorated the spatial memory impairment.
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Animal Model:Female SCID mice (bearing MDA-MB-231 cells)[2]
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Dosage:25 mg/kg
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Administration:I.p.; qd; day 73 post-tumor injection
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Result:Significantly reduced numbers of nodules and lung weights.
Chemical Information
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No. CAS 2151853-97-1
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Appearance Solid
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Peso molecular 293.32
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Fòrmula C17H15N3O2
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Color Light yellow to yellow
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SMILES
O=C(NO)C1=CC=C(CNC2=C3N=CC=CC3=CC=C2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (340.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4092 mL | 17.0462 mL | 34.0925 mL | 85.2311 mL |
| 5 mM | 0.6818 mL | 3.4092 mL | 6.8185 mL | 17.0462 mL | |
| 10 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL | 8.5231 mL | |
| 15 mM | 0.2273 mL | 1.1364 mL | 2.2728 mL | 5.6821 mL | |
| 20 mM | 0.1705 mL | 0.8523 mL | 1.7046 mL | 4.2616 mL | |
| 25 mM | 0.1364 mL | 0.6818 mL | 1.3637 mL | 3.4092 mL | |
| 30 mM | 0.1136 mL | 0.5682 mL | 1.1364 mL | 2.8410 mL | |
| 40 mM | 0.0852 mL | 0.4262 mL | 0.8523 mL | 2.1308 mL | |
| 50 mM | 0.0682 mL | 0.3409 mL | 0.6818 mL | 1.7046 mL | |
| 60 mM | 0.0568 mL | 0.2841 mL | 0.5682 mL | 1.4205 mL | |
| 80 mM | 0.0426 mL | 0.2131 mL | 0.4262 mL | 1.0654 mL | |
| 100 mM | 0.0341 mL | 0.1705 mL | 0.3409 mL | 0.8523 mL |
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