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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M8937 | CPI-455 HCl | CPI-455 HCl is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells, with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays. |
| M6259 | CP2 | CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively. |
| M6143 | SP2509 | SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. |
| M5762 | Mebhydrolin napadisylate | Mebhydrolin (napadisylate) is an antihistamine, used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis. |
| M5229 | EPZ020411 | EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8. IC50 value: 10 nM |
| M5213 | ORY-1001 | ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease. |
| M5212 | GSK2879552 | GSK2879552 is a potent, selective, orally bioavailable, mechanism-based irreversible inactivator of LSD1. |
| M5149 | GSK-J4 | GSK-J4 is a cell permeable procompound rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. |
| M5136 | GSK-LSD1 | 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). |
| M2731 | GSK J4 hydrochloride | 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. |
| M2275 | JIB-04 | JIB-04 is a selective inhibitor of Jumonji histone demethylase with IC50 values of 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. |
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