GSK-J4

N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-ß-alanine ethyl ester

GSK-J4 is a histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC₅₀ = 9 µM for the inhibition of TNFa release). Cell permeable, ethyl ester of GSK-J1. Rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies. Inhibits the growth of T-cell acute lymphoblastic leukemia (T-ALL) cells.

Physical Properties: Yellow wax

MW=417.5 C₂₄H₂₇N₅O₂

Analysis: >99% (TLC); NMR (Conforms)

Solubilization: May be dissolved in DMSO (40 mg/ml); or ethanol (40 mg/ml)

Storage: Store, as supplied, at -20°C. Store solutions at -20°C for up to 3 months.

Amount: 5mg