Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell-permeable GSK-J1 (Cat. No. 420204) prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-A production in primary human macrophage cultures (IC₅₀ = 9 µM by ELISA).r>This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).

The H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]_t=0 = 30 µM; [cellular GSK-J1]_t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC₅₀ = 9 µM by ELISA), in primary human macrophage cultures.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.

Warning

Toxicity: Standard Handling (A)