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1431304-21-0 ORY-1001 (RG-6016, Ladademstat) 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



1639358-50-1 CBB3001 (CBB-3001) is a novel potent, selective histone demethylase LSD1 inhibitor with IC50 of 21.25 uM; potently inhibits LSD1 activity both in vitro and in vivo; CBB3001 also selectively inhibits the growth of human ovarian teratocarcinoma PA-1 and mouse embryonic carcinoma F9 cells, caused the downregulation of pluripotent stem cell proteins SOX2 and OCT4, does not have significant inhibition on the growth of human colorectal carcinoma HCT116 cells or mouse fibroblast NIH3T3 cells that do not express these stem cell proteins.


1222800-79-4 ML324 is a potent, selective JMJD2 demethylase (KDM4) inhibitor with IC50 of 920 nM for JMJD2E, shows no activity against LSD1 (>100-fold selectivity); causes depression-like phenotype even in absence of stress exposure, which is associated with an increase in transcriptionally repressive epigenetic marks H3K9me2/me3 in nucleus accumbens (NAc); blocks TNF-α-mediated neutrophil adhesion, reduces TNF-α-induced ICAM1 protein expression in cerebral microvessels.


1423715-09-6 SP2509 is a potent, selective histone demethylase LSD1 (KDM1A) inhibitor with IC50 of 13 nM, shows no activity against MAOA, MAOB, LDH and glucose oxidase; inhibits the colony growth of OCI-AML3 significantly more than of the other AML cell-types, induces more apoptosis of AML cells expressing mutant NPM1 than mixed-lineage leukemia fusion oncoproteins; significantly improves the survival of immune-depleted mice model of AML, SP2509 is synergistically lethal against cultured and primary AML blasts combined with panobinostat.


5852-78-8 IOX1 is a potent, broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, with IC50 of <1 uM gainst the KDM3, KDM4 and KDM6, 5-25 uM against the KDM5 and KDM2/7; IOX1 is less potent against BBOX1 (IC50=196 uM); chelates to Fe(II) in the active site of 2OG oxygenases; suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II.

L-α-Hydroxyglutaric acid disodium salt

63512-50-5 L-α-Hydroxyglutaric acid disodium salt (L-2-Hydroxyglutarate;L-2-HG) competitive inhibitor of multiple α-KG-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases; comptes with α-KG and inhibits KDM5B/JARID1B/PLU-1 with Ki of 0.628 mM; binds and inhibits ATP synthase and inhibit mTOR signaling in IDH1 mutant cells.


1591932-50-1 Bizine is a phenelzine analog that inhibits LSD1 with Ki of 59 nM, displays 23-fold, 63-fold, and >100-fold selectivity for LSD-1 over MAOA, MAOB, and LSD2 respectively; induces bulk histone H3 lysine 4 dimethylation in LNCaP cancer cells (EC50=2 uM), and protects neurons exposed to oxidative stress at 0.5 uM.

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