JIB04 是一种 Jumonji 组蛋白去甲基酶广谱抑制剂，能抑制 JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C 和 JMJD2D 的活性，其IC50值分别为 230、340、855、445、435、1100 和 290 nM。

JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.

在H358和A549小鼠异种移植模型中,JIB-04抑制Jumonji组蛋白脱甲基酶的活性,抑制肿瘤细胞生长.

在肺癌和前列腺癌细胞系中（IC50=10 nM）,JIB-04下调增殖基因,阻断细胞生长。

For cell viability assays, cells are plated at 1500-3000 cells/well in 96 well plates and treated the next day with increasing doses of compound over 4 days and their viability assessed by standard MTS assays using Promega’s Cell Titer or Cell Titer-Glo reagents according to the manufacturer’s protocols. Absorbance at 490 nm and 650 nm or luminescence is measured by a Spectra Max or a FlouroStar Omega plate reader. Data are normalized to the untreated controls (100% viability). Each cell line is tested in 2-5 independent assays, each containing 4-8 replicates. IC50 values are calculated using DIVISA, a high-throughput software, developed in hous, for storing and analyzing drug sensitivity assays. Dose-response curves are plotted using a non-linear regression model and IC50s are determined from the fitted curves. The average IC50 derived from 2-5 independent assays, each containing 4-8 replicates is reported. (Only for Reference)

199596-05-9

C17H13ClN4

308.77

NSC 693627;5-氯-2(1H)-吡啶酮 (2E)-(苯基-2-吡啶基亚甲基)腙;JIB 04

DMSO:30.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years