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Histone Demethylase

Histone Demethylase

Histone methylation is carried out by methyltransferases and demethylases, two classes of enzymes. While methyltransferases are in charge of creating methylation patterns, demethylases have the ability to remove methyl groups from proteins other than histones. Histone demethylases interact with methylated sites on non-histone proteins, such as p53, in addition to targeting methylated sites on histone tails.
Due to their regulatory functions in chromatin organization and their close ties to diseases like cancer and mental disorders, histone lysine demethylases (KDMs) are of interest as drug targets.

Demethylase JMJD1A, also known as KDM3A, eliminates methyl from histone lysine H3K9. It is crucial for many cellular functions, such as spermatogenesis, energy metabolism, stem cell control, and gender expression.

A histone demethylase known as Jumonji domain-containing 3 (Jmjd3) has been discovered, and it specifically catalyzes the removal of methylation from H3K27me3.

Histone Demethylase related products

Structure Cat No. Product Name CAS No. Product Description
KDOAM-25 trihydrochloride V80481 KDOAM-25 trihydrochloride KDOAM-25 tri HCl is a potent and selective inhibitor of histone lysine demethylase 5 (KDM5), with IC50s of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D respectively.
LSD1-IN-22 V75854 LSD1-IN-22 2821068-05-5 LSD1-IN-22 is a potent lysine-specific demethylase 1 (LSD1) inhibitor (antagonist) with a Ki of 98 nM.
LSD1-IN-23 V79972 LSD1-IN-23 LSD1-IN-23 is a mixed competitive/noncompetitive inhibitor of lysine-specific demethylase 1 LSD1.
LSD1-IN-24 V51842 LSD1-IN-24 4734-59-2 LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor (antagonist) with IC50 = 0.247 μM.
LSD1-IN-25 V51841 LSD1-IN-25 2911585-60-7 LSD1-IN-25 (Compound 9j) is a specific, orally bioactive LSD1 inhibitor (antagonist) with IC50 of 46 nM (Ki = 30.3 nM).
LSD1-IN-26 V80623 LSD1-IN-26 LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor (antagonist) with IC50 of 25.3 nM.
LSD1-IN-27 V56072 LSD1-IN-27 2904571-94-2 LSD1-IN-27 (Compound 5ac) is an LSD1 inhibitor (IC50= 13 nM).
LSD1-IN-29 V85325 LSD1-IN-29 1496573-83-1
LSD1-IN-30 V85462 LSD1-IN-30 1289575-45-6
LSD1-IN-31 V88881 LSD1-IN-31 LSD1-IN-31 (compound 11e) can directly bind to the LSD1/CoREST complex and reduce the demethylase activity of LSD1.
LSD1-IN-33 V101167 LSD1-IN-33 LSD1-IN-33 (7d) is an orally active LSD1 inhibitor (IC50 of 4.51 nM) that attenuates Ang II-induced NRCF activation and reduces TAC-induced cardiac remodeling and pathological myocardial remodeling in heart failure.
LSD1-IN-34 V99929 LSD1-IN-34 LSD1-IN-34 (compound 7d) is an oral lysine-specific demethylase (LSD) and monoamine oxidase (MAO) inhibitor with IC50 of 4.51 and 18.46 nM for LSD1 and MAO A, respectively.
LSD1-IN-35 V96694 LSD1-IN-35 2992690-04-5 LSD1-IN-35 (Compound Z-1) is a selective LSD1 inhibitor (IC50: 108 nM).
LSD1-IN-37 V103677 LSD1-IN-37 LSD1-IN-37 (compound 5g) is a lysine-specific demethylase 1 (LSD1) inhibitor constructed through an efficient hexafluoroisopropyl-containing synthetic strategy. This method does not require a metal catalyst, has good reaction stability and adaptability, exhibits excellent LSD1 inhibitory activity, and has the potential for further research.
LSD1-IN-38 V105034 LSD1-IN-38 LSD1-IN-38 (Compound 23e) is a reversible, orally active lysine-specific demethylase 1 (LSD1) inhibitor with IC50 of 1.2 nM.
LSD1-UM-109 V56073 LSD1-UM-109 2252446-26-5 LSD1-UM-109 is a potent and reversible inhibitor of LSD1 with IC50 of 3.1 nM.
LSD1/2-IN-3 V75859 LSD1/2-IN-3 2821068-07-7 LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with a Ki of 11 nM and a Ki of 7 μM for LSD2.
LSD1/2-IN-4 V75858 LSD1/2-IN-4 2821068-09-9 LSD1/2-IN-4 is a PCPan analogue and an inhibitor (blocker/antagonist) of LSD1 and LSD2.
LSD1/EGFR-IN-1 V104387 LSD1/EGFR-IN-1 336171-65-4 LSD1/EGFR-IN-1 (Compound L-1) is a potent inhibitor of LSD1, EGFR T790M/L858R, and EGFR L858R/T790M/C797S with IC50 of 6.24, 2.06, and 5.01 μM, respectively.
LSD1/HDAC6-IN-1 V51843 LSD1/HDAC6-IN-1 2738306-38-0 LSD1/HDAC6-IN-1 is an orally bioactive dual (bifunctional) inhibitor of histone demethylase LSD1 and histone deacetylase HDAC6 (LSD1/HDAC6) with anti-tumor activity.
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