| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
HDAC6 0.291 μM (IC50)
HDAC6 (histone deacetylase 6). MPT0G211 inhibits HDAC6 with high potency and selectivity. It disrupts the deacetylation of non-histone proteins such as α-tubulin and Hsp90, affecting protein trafficking and stress responses in cancer cells. |
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| ln Vitro |
The phosphorylation of tau Ser396 is greatly inhibited by MPT0G211 (0.1 μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 hours)[1]. Inhibiting HDAC6/Hsp90 binding, MPT0G211 leads to the proteasomal breakdown of polyubiquitinated proteins[1]. Tau phosphorylation is markedly reduced by MPT0G211 through GSK3β inactivation[1]. h using pRK5-EGFP-Tau P301L and pCAX APP 695)[1]. The proliferation of MDA-MB-231 and MCF-7 cells is inhibited by MPT0G211 (GI50 = 16.19 and 5.6 μM, respectively)[2]. Through the inhibition of DNA repair mechanisms and the activation of Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis, MPT0G211 enhanced the cytotoxic effects of DOXO in AML cells[3].
MPT0G211 inhibits HDAC6 with an IC50 of 0.291 nM and is >1000-fold selective over other HDAC isoforms. It has shown anti-metastatic activity in human breast cancer cells. Detailed cellular activity data is available from specialized databases. |
| ln Vivo |
The impairment in spatial memory is greatly improved by MPT0G211 (50 mg/kg; po; daily for 3 months)[1]. MPT0G211 (ip; qd; day 73 post-tumor injection; 25 mg/kg) decreases lung weights and nodule counts[2]. In addition to reducing tau phosphorylation by blocking GSK3β activity, MPT0G211 therapy increases Hsp90's acetylation, which downregulates HDAC6/Hsp90 binding and speeds up the proteasomal breakdown of polyubiquitinated p-tau[1].
MPT0G211 is orally active and has shown anti-metastatic activity in vivo. It has neuroprotective effects. It is active in animal models and has a favorable pharmacokinetic profile. It is used in cancer and neurodegenerative disease research. |
| Enzyme Assay |
In vitro enzyme assays are performed using recombinant HDAC6 and a fluorogenic substrate (e.g., Boc-Lys(Ac)-AMC). The enzyme is incubated with the substrate and the compound, and the fluorescence signal is measured to calculate IC50 values.
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| Cell Assay |
Cells (e.g., breast cancer cells) are treated with MPT0G211. Cell viability is measured using MTT or CellTiter-Glo assays. Acetylation of α-tubulin and Hsp90 is measured by Western blotting. Cell migration and invasion are assessed using transwell or scratch assays.
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| Animal Protocol |
Animal/Disease Models: Triple transgenic (3×Tg-AD) mice (harboring APPSwe and tauP301L mutant transgenes[1]
Doses: 50 mg/kg Route of Administration: Po; daily for 3 months Experimental Results: Dramatically ameliorated the spatial memory impairment. Animal/Disease Models: Female SCID (severe combined immunodeficient) mouse (bearing MDA-MB-231 cells)[2] Doses: 25 mg/kg Route of Administration: Ip; qd; day 73 post-tumor injection Experimental Results: Dramatically diminished numbers of nodules and lung weights. In vivo efficacy studies are performed in mouse models of cancer (e.g., breast cancer metastasis models) or neurodegenerative diseases. MPT0G211 is administered orally. Tumor growth or metastasis is monitored. Neuroprotective effects are assessed using behavioral tests and histology. Biomarkers (e.g., acetylated α-tubulin) are measured in tissues. |
| ADME/Pharmacokinetics |
MPT0G211 is orally active. It has a molecular weight of 293.32 and a molecular formula of C17H15N3O2. It is soluble in DMSO. Detailed pharmacokinetic parameters such as oral bioavailability and half-life are available from specialized databases. It is stored at -20°C.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles of MPT0G211 are not extensively reported. In vivo studies show that it is tolerated at efficacious doses. As a selective HDAC6 inhibitor, it is expected to have fewer toxicities than pan-HDAC inhibitors, which are associated with hematological and gastrointestinal side effects.
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| References |
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| Additional Infomation |
MPT0G211 is a research-grade HDAC6 inhibitor. It is used in cancer and neurodegenerative disease research. It is not approved for clinical use. Its molecular formula is C17H15N3O2 and its molecular weight is 293.32.
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| Molecular Formula |
C17H15N3O2
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|---|---|
| Molecular Weight |
293.319903612137
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| Exact Mass |
293.116
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| CAS # |
2151853-97-1
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| Related CAS # |
MPT0G211 mesylate;2151854-33-8
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| PubChem CID |
132157820
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
369
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(=CC=1)CNC1=CC=CC2=CC=CN=C12)NO
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| InChi Key |
BPDQUKCPNSRTTR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N3O2/c21-17(20-22)14-8-6-12(7-9-14)11-19-15-5-1-3-13-4-2-10-18-16(13)15/h1-10,19,22H,11H2,(H,20,21)
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| Chemical Name |
N-hydroxy-4-[(quinolin-8-ylamino)methyl]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (340.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4092 mL | 17.0462 mL | 34.0925 mL | |
| 5 mM | 0.6818 mL | 3.4092 mL | 6.8185 mL | |
| 10 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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