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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M21313 | Pulrodemstat | Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine-specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. |
| M21127 | TAK-418 | TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. It is an orally administered CNS-permeable clinical candidate for the study of neurodevelopmental disorders, such as autism spectrum disorders. |
| M20864 | L-2-Hydroxyglutaric acid disodium | L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively. |
| M15089 | PBIT | PBIT is a JARID1 (Jumonji AT-Rich Interactive Domain 1) inhibitor with IC50 values of 3, 4.9 and 6 μM for JARID1B, 1A and 1C, respectively. It can increase trimethylation of H3K4 in HeLa cells and block the proliferation of tumor cells expressing high levels of JARID1B. |
| M13838 | Seclidemstat mesylate | Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). |
| M13837 | NCGC00244536 | NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM. |
| M13836 | KDM5-IN-1 | KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM. |
| M13835 | KDM5A-IN-1 | KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. |
| M13834 | KDM4D-IN-1 | KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM. |
| M13832 | GSK467 | GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members. |
| M13829 | GSK 690 Hydrochloride | GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM. |
| M10921 | GSK2879552 dihydrochloride | GSK2879552 dihydrochloride is an oral, irreversible LSD1/KDM1A inhibitor with antitumor activity. |
| M10826 | GSK 690 Hydrochloride | GSK 690 (Hydrochloride) is a reversible inhibitor of lysine-specific demethylase 1 (LSD1),Kd The value is 9 nM,IC50 The value is 37 nM. |
| M10727 | Pulrodemstat benzenesulfonate | CC-90011 (Pulrodemstat) benzenesulfonate is a potent, selective, reversible and orally active lysine-specific demethylase-1 (LSD1) inhibitor,IC50 0.25 nM. CC-90011 benzenesulfonate has less enzymatic inhibition of LSD2, MOA-A and MAO-B. CC-90011 benzenesulfonate induces differentiation of acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells and has potent anti-cancer activity. |
| M9689 | Seclidemstat | Seclidemstat is an orally active, reversible, noncompetitive inhibitor of lysine-specific demethylase 1 (LSD1, or KDM1A) with a mean IC50 of 127 nM, it has potential antineoplastic activity. |
| M9644 | T-3775440 hydrochloride | T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM. |
| M9526 | GSK-J5 | GSK-J5 is a cell-permeable, inactive control for histone demethylase JMJD3/UTX inhibitor GSK-J4. |
| M9375 | QC6352 | QC6352 is a potent KDM4C inhibitor. |
| 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. |
| M6831 | IOX1 | IOX1 is a histone demethylase inhibitor; cell permeable. IOX1 also inhibits ALKBH5. |
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