Methylstat (hydrate) Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 IC
50 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 GI
50 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 (EC
50 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 (hydrate) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte