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FB23-2 is a potent, selective inhibitor of the mRNA N 6-methyladenosine (m 6A) demethylase FTO, directly bind to FTO, inhibits FTO demethylation of m6 A in RNA in vitro with IC50 of 2.6 uM; demonstrates significantly improved anti-proliferative activity on NB4 and MONOMAC6 cells with IC50 of 0.8-1.5 uM, compared with parental compound FB23; dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro; FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.


ORY-1001 trans and cis isomers


ORY-1001 (RG-6016) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.

Blood Cancer

Phase 2 Clinical




QC-6352 is a potent and selective KDM4 family inhibitor with IC50 of 104, 56, 35, and 104 nM for KDM4A, KDM4B, KDM4C, and KDM4D, respectively; displays high selectivity over other KDM family members, with the exception of KDM5B (IC50=750 nM); shows a promising cellular potency (KYSE-150 EC50=3.5 nM, H3K36 MOA=1.5 nM); has excellent physical properties and drug-like characteristics, exhibits favorable in vivo efficacy in a breast cancer PDX model and reduces the tumor initiating cell populations which are associated with resistance to chemotherapy treatments.




Seclidemstat (SP-2577, SP2577) is a potent, selective LSD1 inhibitor with IC50 of 127 nM, reduces tumor volume in vivo.




T-3775440 is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM; displays high selectivity for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B); disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B) in leukemia cell lines, exhibites significant antitumor efficacy in AEL and AMKL xenograft models.




KDOAM-25 (KDM5 inhibitor KDOAM 25) is a potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively; weakly inhibits KDM4C/KDM2B (IC50=4.8/4.4 uM) and good selectivity over other demethylases; most potently inhibits KDM5B (IC50=50 uM) and increases H3K4me3 levels in Hela cells; increases global H3K4 methylation, causes G1 cell-cycle arrest and impairs cell proliferation in multiple myeloma MM1S cells.


T-448 free base

1597426-52-2 T-448 free base (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation.

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