JIB-04

(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine

JIB-04 is a novel specific inhibitor of the Jumonji family of histone demethylases in vitro, in cancer cells and in tumors in vivo. IC₅₀ = 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. Reduces tumor burden and prolongs life in a mouse model. Suppresses translation initiation and enhances mTOR inhibitor sensitivity. Inhibits the growth of temozolomide-resistant glioblastoma cells and crosses the blood brain barrier.

Physical Properties: Yellow powder

MW= 308.8 C₁₇H₁₃ClN₄

Analysis: >98% (TLC); NMR (Conforms)

Solubilization: May be dissolved in DMSO (30 mg/ml)

Storage: Store desiccated as supplied at -20°Ctemperature for up to 2 years. Store solutions at -20°C for up to two months.

Amount: 5 mg