JIB-04 (NSC 693627),E JIB-04;JIB-04 (NSC 693627);JIB04/JIB-04;5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone;5-Chloro-2-[(E)-2-[phenyl(pyridin-2-yl)methylidene]hydrazin-1-yl]pyridine;NSC 693627;5-Chl 199596-05-9
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
IC50 Value: 230 nM (for JARID1A); 340 nM (for JMJD2E); 855 nM (for JMJD3) 445 nM (for JMJD2A); 435 nM (for JMJD2B); 1100 nM (for JMJD2C); 290 nM (for JMJD2D) [1]
Target: Jumonji Histone Demethylase
in vitro: JIB-04 induces transcriptional changes in a cancer-selective manner, including the downregulation of proliferative genes and the upregulation of the anti-proliferative/pro-apoptotic genes. JIB-04 blocks growth of lung and prostate cancer lines with IC50 as low as 10 nM, while produces less anti-proliferative activities on HBECs and PrSCs/PrECs [1].
in vivo: In two separate xenograft mouse models (H358 or A549), JIB-04 diminishes tumor growth, lowers Jumonji histone demethylase activity in tumors, and prolongs cancer survival [1].
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