jmjd3

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

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).

Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].

KDM4-IN-2 is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.

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

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.

GSK-J1 sodium salt is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX.

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].

GSK-J2 sodium, the sodium form of GSK-J2, is an isomer of GSK-J1 and lacks specific activity. GSK-J1 is a potent inhibitor of H3K27me3 me2-demethylases JMJD3 KDM6B and UTX KDM6A [1].