Methylstat

TargetMol Chemicals

Methylstat

9

1310877-95-2

Chemical

Methylstat

C28H31N3O6

505.56

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 uM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 uM, whereas the free acid of methylstat did not inhibit cell growth up to 100 uM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 uM in KYSE150 cells and 6.7 ad 6.3 uM in MCF-7 cells, respectively).

3 years

N(C(OCC1=CC=C(CNCCCCN(C(/C=C/C(OC)=O)=O)O)C=C1)=O)C=2C3=C(C=CC2)C=CC=C3

-20°

12352200