phf8

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).

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2 7 JmjC subfamily.

JHDM-IN-1 (Compound 1), a Jumonji C domain-containing HDMs (JHDM) inhibitor, exhibits IC50s of 3.4 μM against JMJD2C, 4.3 μM against JMJD2A, 5.9 μM against JMJD2E, 10 μM against PHF8, and 43 μM against JMJD3, showcasing its inhibitory effectiveness across a spectrum of JHDM enzymes [1].

Daminozide-d6 (dimethyl-d6) is a deuterated compound of Daminozide. Daminozide has a CAS number of 1596-84-5. Daminozide is a plant growth regulator, selectively inhibits the KDM2 7 JmjC subfamily.