Methylstat (hydrate)

Methylstat (hydrate)

CAT N°: 11091
Price:

From 80.00 68.00

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.{19980} 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).

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2E-butenoic acid, methyl ester, hydrate
  • Correlated keywords
    • JMJD2A JMJD2C JMJD2E JMJD-2A JMJD-2C JMJD-2E JmjC PHF-8 pro-drug Jumonji C domain-containing histone demethylase methylation hyper-methylation 1310877-95-2
  • Product Overview:
    Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.{19980} 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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