Histone Demethylase
There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.
Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.
JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.
Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.
Histone Demethylase Isoform Specific Products
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Histone Demethylase Inhibitors
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Histone Demethylase Antagonist
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Histone Demethylase Activators
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Histone Demethylase Degraders
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Histone Demethylase Controls
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Histone Demethylase Ligands
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Histone Demethylase Related Products (297)
Related Products (297)
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Antibodies (8)
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Histone Demethylase Isoform Comparison
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Seclidemstat (Standard)
0 ImagesCat. No.: HY-103713RCAS No.: 1423715-37-0Synonyms: SP-2577 (Standard)Seclidemstat (Standard) is the analytical standard of Seclidemstat (HY-103713). This product is intended for research and analytical applications. Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.
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Daminozide (Standard)
0 ImagesDaminozide (Standard) is the analytical standard of Daminozide. This product is intended for research and analytical applications. Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested.
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QC6352 (Standard)
0 ImagesCat. No.: HY-104048RCAS No.: 1851373-36-8QC6352 (Standard) is the analytical standard of QC6352 (HY-104048). This product is intended for research and analytical applications. QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B).
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CBB1003
0 ImagesCat. No.: HY-15774CAS No.: 1379573-88-2CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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CBB3001
0 ImagesCat. No.: HY-124616CAS No.: 1639358-50-1CBB3001 is an inhibitor of LSD1/KDM1A. CBB3001 exerts its effect by inhibiting Histone Demethylase activity, with an IC50 of 21.25 μM. It downregulates the expression of pluripotency-related proteins and genes such as SOX2 and OCT4, and induces cell differentiation, growth arrest, and apoptosis. CBB3001 can be used for research on testicular germ cell tumors, teratomas, and embryonal carcinomas.
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Eicosapentaenoic acid metformin
0 ImagesCat. No.: HY-B0660ACAS No.: 1384526-74-2Synonyms: EPA metformin; Timnodonic acid metforminEicosapentaenoic Acid (EPA) metformin is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic acid metformin exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). EEicosapentaenoic acid metformin activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic acid metformin can promote relaxation of vascular smooth muscle cells and vasodilation.
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RN-1 dihydrochloride (Standard)
0 ImagesCat. No.: HY-110130RCAS No.: 1781835-13-9RN-1 dihydrochloride (Standard) is the analytical standard of RN-1 (dihydrochloride) (HY-110130). This product is intended for research and analytical applications. RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively.
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LSD1-IN-44
0 ImagesCat. No.: HY-175184LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC50 of 0.02 μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research.
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MC3935
0 ImagesCat. No.: HY-175185MC3935 is a LSD1 inhibitor with an IC50 of 0.52 μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.
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OG-L002 hydrochloride
0 ImagesCat. No.: HY-19333ACAS No.: 1357299-45-6OG-L002 hydrochloride is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 hydrochloride is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 hydrochloride potently inhibits the expression of HSV IE genes.
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T-3775440 hydrochloride (Standard)
0 ImagesCat. No.: HY-103085RCAS No.: 1422535-52-1T-3775440 hydrochloride (Standard) is the analytical standard of T-3775440 hydrochloride (HY-103085). This product is intended for research and analytical applications. T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
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KDM5-IN-1 (Standard)
0 ImagesCat. No.: HY-100422RCAS No.: 1628210-26-3KDM5-IN-1 (Standard) is the analytical standard of KDM5-IN-1 (HY-100422). This product is intended for research and analytical applications. KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
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GSK-LSD1 dihydrochloride (Standard)
0 ImagesCat. No.: HY-100546ARCAS No.: 2102933-95-7GSK-LSD1 (dihydrochloride) (Standard) is the analytical standard of GSK-LSD1 (dihydrochloride) (HY-100546A). This product is intended for research and analytical applications. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
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HDM-IN-1
0 ImagesCat. No.: HY-169919CAS No.: 3020690-76-7HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model.
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KDM5A-IN-1 (Standard)
0 ImagesKDM5A-IN-1 (Standard) is the analytical standard of KDM5A-IN-1 (HY-100014). This product is intended for research and analytical applications. 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. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
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N-Oxalylglycine (Standard)
0 ImagesN-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively.
