MilliporeSigma™ Calbiochem™ JHDM Inhibitor VII, JIB-04

Description

A cell-permeable, selective inhibitor of Jumonji family histone demethylases (IC₅₀ = 230 to 1100nM)

The E-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against Jumonji family histone demethylases (IC₅₀ = 230, 290-320, 340, 435, 445, 855, and 1,100 nM, respectively, against JARID1A/KDM5A, JMJD2D/KDM4D, JMJD2E/KDM4E, JMJD2B/KDM4B, JMJD2A/KMD4A, JMJD3/KDM6B, and JMJD2C/KDM4C, respectively), presumably via catalytic site iron interaction, displaying little toward 5mC DNA hydroxylase TET1, aurora kinases, HDACs, HIF prolyl hydroxylase PHD2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase LSD1/KDM1A. Shown to exhibit anticancer activity against H358 and A549 lunger cancer cells both in cultures in vitro (IC₅₀ in 4 d = 100 and 250 nM, respectively) and in mice in vivo (via i.p. at 100mg/kg and p.o. at 55mg/kg, respectively; 2-3 times per week).

Specifications

• Color: Light Beige
• Description: 98% by HPLC
• Target Proteins: Jumonji family of histone demethylases
• CAS: 199596-05-9
• Molecular Formula: C₁₇H₁₃ClN₄
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 10 mg