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Methylstat

Catalog No. T7057 CAS 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).

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Methylstat, CAS 1310877-95-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Targets&IC50

JMJD2A:4.3 µM, PHF8:10 µM , JMJD2E:5.9 µM, JMJD3:43 µM, JMJD2C:3.4 µM

Molecular Weight	505.571
Formula	C28H31N3O6
CAS No.	1310877-95-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 25 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Luo, X., et al. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. Journal of the American Chemical Society 133(24), 9451-9456 (2011).

Related Products

Related compounds with same targets

Methylstat Eicosapentaenoic Acid KDM2B-IN-2 GSK2879552 CP2 CPI-455 HCl KF21213 S2101

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Keywords

Methylstat 1310877-95-2 表观遗传其他 Histone Demethylase Others anti-proliferative HUVECs anti-angiogenic G0/G1 phase Apoptosis p53 Inhibitor MDM-2/p53 low cytotoxicity inhibit inhibitor

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