JQKD82, also known as PCK82, is a cell-permeable and selective KDM5 inhibitor (MM.1S cells, IC50 = 0.42 uM). JQKD82 increases histone H3K4me3 but paradoxically inhibits downstream MYC-driven transcriptional output in vitro and in vivo. JQKD82 is a useful tool compound to block KDM5A function as a potential therapeutic strategy for MM. QKD82 is a more stable ester of KDM5-C49 that is able to deliver the active molecule KDM5-C49 to cells more efficiently
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma[1].
JQKD82 (50-75 mg/kg; i.p.; twice a day for 3 weeks) has anti-multiple myeloma activity[1].
JQKD82 displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo[1].
| Animal Model: | Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells)[1] |
| Dosage: | 50 mg/kg, 75 mg/kg |
| Administration: | i.p.; twice a day for 3 weeks |
| Result: | Significantly reduced tumor burden.
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KDM5 inhibitor (MM.1S cells, IC50 = 0.42 uM)
[1] Jun Qi, et al. Histone demethylase 5 inhibitors and uses thereof. WO2020033377A1.
![4-Pyridinecarboxylic acid, 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-, 2,4-bis(1-methylethoxy)phenyl ester Structure](/CAS/20211123/GIF/2410512-38-6.gif)
