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Histone demethylase Histone demethylase

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.
M28639 Bizine  Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects.
M28481 KDM2/7-IN-1  KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro.
M28239 Vafidemstat Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
M28017 NCDM-32B  NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
M27960 KH-3  KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction.
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.

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.
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.




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