JIB-04, pan-JUMONJI histone demethylase inhibitor

Product Details

Formal Name: (E)-5-Chloro-2-(2-(phenyl(pyridine-2-yl)methylene)hydrazinyl)pyridine

Molecular Formula: C₁₇H₁₃ClN₄

Formula Weight: 308.76

CAS Number: 199596-05-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 30 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

pan-JUMONJI histone demethylase inhibitor

Functions

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.

Application Procedures

First dissolved in DMSO (up to 30 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)