JIB-04

Research use only, not for human use.

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

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 is consistently selective for cancer vs. normal cells, demonstrated by the higher sensitivity of lung and prostate cancer lines (with IC50?as low as 10 nM) compared to HBECs and PrSCs/PrECs. JIB-04 inhibits cellular Jumonji demethylase activity, and Jumonji levels affect JIB-04 action in cells. JIB-04 significantly inhibits the proliferation of GB cell lines and stem-enriched cultures. JIB-04 exerts its maximal inhibitory activity against KDM5A, and modulates the expression of genes involved in the control of cancer cell growth and leads to hypermethylation of H3K4. Furthermore, JIB-04 (2500 nM) activates the autophagy and apoptotic pathways and inactivates PI3K. JIB-04 also cooperates with TMZ in killing GB cells.

JIB-04 results in a significant reduction in cancer-induced death rates in mice, prolonging survival. JIB-04 (60, 40 and 20 mg/kg, i.p.) reaches bioactive concentration in the brain of the mice. The orthotopic GB xenograft model shows a trend toward longer survival in JIB-04-treated mice with an Hazard Ratio of 0.5.

JHDM Inhibitor VII | NSC 693627

Chromatin/Epigenetic

Histone Demethylase

JMJD2A| JMJD2B| JMJD2D| JMJD2E| JARID1A

Cancer

——

199596-05-9

308.76

C17H13ClN4

>98% (HPLC)

DMSO: 25 mg/mL warmed (80.96 mM)

ClC1=CN=C(N/N=C(C2=CC=CC=C2)/C3=NC=CC=C3)C=C1

(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine

(-20℃)

With Ice Pack

≥ 2 years