- KDM1
- KDM2
- KDM3
- KDM4
- KDM5
- KDM6
KDM5 选择性抑制剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| S0269 | GSK467 | GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members. | Selective | KDM5B, Ki: 10 nM |
| S8287 | CPI-455 HCl | CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. | Selective | KDM5A, IC50: 10 nM |
| S6389 | CPI-455 | CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes. |
Pan | KDM5, IC50: 10 nM |
| S7281 | JIB-04 | JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively. JIB‑04 also induces cell apoptosis. | Pan | JARID1A, IC50: 230 nM |
| S0201 | Z-JIB-04 (NSC 693627) | Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. | Pan | JARID1A, IC50: 230 nM |
| S7234 | IOX1 | IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5. | Pan | KDM5C, IC50: 19 μM |
