| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
HDAC6 0.291 μM (IC50)
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|---|---|
| ln Vitro |
The phosphorylation of tau Ser396 was considerably reduced by MPT0G211 mesylate (0.1 μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 hours)[1]. The inhibition of HDAC6/Hsp90 binding by MPT0G211 mesylate leads to the subsequent proteasomal degradation of proteins that are polyubiquitinated [1]. By inactivating GSK3β, MPT0G211 mesylate dramatically reduces tau phosphorylation[1]. were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for a duration of 24 hours[1]. The proliferation of MDA-MB-231 and MCF-7 cells is inhibited by MPT0G211 mesylate (GI50 = 16.19 and 5.6 μM, respectively)[2]. MPT0G211 mesylate increases the cytotoxic effects of DOXO in AML cells by causing damage to the machinery that repairs DNA and triggering cell apoptosis that is dependent on Bcl-2-associated X protein (BCL-XL)[3].
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| ln Vivo |
The spatial memory impairment is greatly improved by MPT0G211 mesylate (50 mg/kg; po; daily for 3 months)[1]. Mesylate (25 mg/kg; intraperitoneal; QD; day 73 post-tumor injection) MPT0G211 decreases lung weights and nodule counts[2]. In addition to reducing tau phosphorylation by blocking GSK3β activity, MPT0G211 mesylate therapy also increases Hsp90's acetylation, which downregulates HDAC6/Hsp90 binding and speeds up the proteasomal breakdown of polyubiquitinated p-tau[1].
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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. |
| 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.
[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. |
| Molecular Formula |
C18H19N3O5S
|
|---|---|
| Molecular Weight |
389.43
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| CAS # |
2151854-33-8
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| Related CAS # |
MPT0G211;2151853-97-1
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| SMILES |
C1(C(NC)=O)=CC=C(CNC2C=CC=C3C=CC=NC=23)C=C1.S(=O)(O)(=O)C
|
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5679 mL | 12.8393 mL | 25.6786 mL | |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1357 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5679 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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