jmjd2a

DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.

JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor.

Selective FTO inhibitor (IC50 = 0.81 μM). Exhibits >30-fold selectivity for FTO over ALKBH2, 3 and 5 and >100-fold selectivity over PHD2 and JMJD2A. Increases levels of modified N6-methyladenosine (m6A) in HeLa cells in a concentration-dependent manner.

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).

Prohexadione is a plant growth regulator. It inhibits the gibberellin plant hormone biosynthesis enzyme 3β-hydroxylase when used at concentrations of 0.1, 1, and 10 mM. It reduces the shoot length of peanut plants when applied at 0.5, 1.5, and 4.5 kg hectare. Prohexadione also inhibits jumonji domain-containing 2A (JMJD2A) demethylase when used at a concentration of 1 mM and induces the differentiation of mouse neurospheres into neurons at 1, 1.5, and 2 mM. Formulations containing prohexadione have been used as plant growth regulators in agriculture.

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].