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Methylstat
🥰Excellent
Catalog No. T7057Cas No. 1310877-95-2
Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).
Methylstat
🥰Excellent
Purity: 98.34%
Catalog No. T7057Cas No. 1310877-95-2
Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $199 | In Stock |
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Purity:98.34%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively). |
| Targets&IC50 | JMJD2A:4.3 µM, JMJD3:43 µM, JMJD2C:3.4 µM, PHF8:10 µM , JMJD2E:5.9 µM |
| Molecular Weight | 505.56 |
| Formula | C28H31N3O6 |
| Cas No. | 1310877-95-2 |
| Smiles | COC(=O)\C=C\C(=O)N(O)CCCCNCc1ccc(COC(=O)Nc2cccc3ccccc23)cc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (49.45 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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