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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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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. |
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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. |
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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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V56069 | MC2652 | 2771425-46-6 | MC2652 (compound 1a) is a potent LSD1 inhibitor. |
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V0375 | ML324 (CID44143209) | 1222800-79-4 | ML324 (also known as CID-44143209) is a cell-permeable and selective inhibitor of jumonji histone demethylase (JMJD2) with antiviral activity. |
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V76737 | MY-943 | MY-943 is a potent inhibitor of tubulin polymerization and LSD1 with anti-cancer activity. | |
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V41137 | Namoline | 342795-11-3 | Namoline, a γ-pyrone, is a selective, reversible inhibitor of lysine-specific demethylase 1 (LSD1) with IC50 of 51 μM in an HRP-conjugating enzyme assay. |
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V80906 | NCD38 TFA | NCD38 TFA is a selective inhibitor of LSD1. | |
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V3301 | NCGC00244536 | 2003260-55-5 | NCGC00244536 (also known as KDM4B Inhibitor B3; KDM4B-IN-B3)is a novel and potent inhibitor of the Histone lysine demethylase KDM4 with anIC50of 10 nM. |
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V0370 | OG-L002 | 1357302-64-7 | OG-L002 (OG-L-002) is a pecific inhibitor of LSD-1 [lysine (K)-specific demethylase 1A] with potential antiviral activity. |
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V27126 | PBIT | 2514-30-9 | PBIT is a specific Jumonji/AT enriched interacting domain 1 (JARID1) inhibitor. |
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V29996 | Procaine (Novocaine) | 59-46-1 | Procaine (also known as Novocaine HCl), the HCl salt of thelocal anesthetic Procaine, is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
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V15540 | Pulrodemstat (CC90011) | 1821307-10-1 | Pulrodemstat (formerly CC-90011; LSD1-IN-7; CC90011) is a novel, highly potent, reversible and orally bioavailable inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity. |
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V40117 | Pulrodemstat (CC90011) besylate | 2097523-60-7 | Pulrodemstat besylate (formerly CC-90011 besylate; LSD1-IN-7), the besylate salt of CC-90011 (LSD1-IN7; CC90011), is a highly potent and orally bioavailable inhibitor of lysine specific demethylase-1 (LSD1) with potential anticancer activity. |
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V52293 | Pulrodemstat Methylbenzenesulfonate (CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate) | 2097523-57-2 | CC-90011 Methylbenzenesulfonate is a specific, reversible and orally bioactive lysine-specific demethylase-1 (LSD1) inhibitor (antagonist) with IC50 of 0.25 nM. |
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V56071 | S1427 | 2447061-40-5 | S1427 is a tranylcypromine-derived LSD1 inhibitor (antagonist) with IC50 of 390 nM and a Ki of 80 nM. |
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V37863 | S2116 | 2262489-89-2 | S2116 is an N-alkylated trans-cyclopropylamine (TCP) analogue and a potent lysine-specific demethylase 1 (LSD1) inhibitor. |
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V37842 | S2157 | 2262488-39-9 | S2157 is an N-alkylated trans-cyclopropylamine (TCP) analogue and a potent lysine-specific demethylase 1 (LSD1) inhibitor. |
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V3833 | Seclidemstat | 1423715-37-0 | Seclidemstat (formerly also known as SP-2577; SP2577) is a novel, potent small molecule inhibitor of epigenetic enzyme LSD1 (lysine-specific demethylase 1) with anticancer activity. |
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V37130 | Seclidemstat mesylate (SP-2577 mesylate) | 2044953-70-8 | Seclidemstat (SP-2577) mesylate is a potent, noncompetitive, reversible inhibitor of KDM1A (LSD1) (Ki=31 nM, IC50). |
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