JIB-04 is a potent, cell-permeable inhibitor of Jumonji histone demethylase in vitro and in vivo (IC50 values are 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively). JIB-04 selectively inhibited viability of several human cancer cell lines with little toxicity towards normal cells, and also diminished tumor growth in two separate xenograft mouse models. JIB 04 selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mg/mL|
|Source||Sci Rep (2018). Figure 1. JIB-04|
|Cell Lines||colorectal cancer cells|
|Concentrations||2 μM, 10 μM|
|Incubation Time||24 hr|
|Results||When we treated HCT116 cells with JIB-04 for 24 h, the cell viability decreased as the concentration of JIB-04 increased, with a maximum reduction in viability of about 50% compared with the viability of the DMSO-treated control cells|
A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.
Wang L, et al. Nat Commun. 2013;4:2035. PMID: 23792809.
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