Size | Price | Stock |
---|---|---|
5mg | $55 | In-stock |
10mg | $88 | In-stock |
50mg | $220 | In-stock |
100mg | $385 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-13953 |
M.Wt: | 308.76 |
Formula: | C17H13ClN4 |
Purity: | >98 % |
Solubility: | Ethanol : 2 mg/mL (6.48 mM; Need ultrasonic); DMSO : 50 mg/mL (161.94 mM; Need ultrasonic) |
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. IC50 & Target: IC50: 230 nM (JARID1A), 445 nM (JMJD2A), 435 nM (JMJD2B), 1100 nM (JMJD2C), 290 nM (JMJD2D), 340 nM (JMJD2E), 855 nM (JMJD3)[1] In Vitro: 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[1]. 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[2]. In Vivo: JIB-04 results in a significant reduction in cancer-induced death rates in mice, prolonging survival[1]. 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[2].
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