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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.
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Source | Sci Rep (2018). Figure 1. JIB-04 |
| Method | Viability assay | |
| 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 |
| Molecular Weight | 308.76 |
| Formula | C17H13ClN4 |
| CAS Number | 199596-05-9 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone demethylase Products |
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| GSK-J1
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. GSK J1 is selective for the H3K27 demethylases JMJD3 and UTX. |
| GSK-J4 hydrochloride
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 hydrochloride is a cell permeable procompound of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family. |
| OG-L002
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
| GSK-LSD1 dihydrochloride
GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). |
| GSK-J4
GSK-J4 is a cell permeable procompound rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. |
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