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Histone demethylases Histone demethylases

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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