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JIB-04 199596-05-9

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Synonyms ：
Appearance ：
Chemical Formula ：
C17H13ClN4
Solubility ：
Molecular Weight ：
308.76
Storage and Stability ：
in stock
CAS No. ：
199596-05-9
Purity ：
98%+
Introduction
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively.

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.

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


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