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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V76952 | GSK-J1 lithium salt | GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM for KDM6B. | |
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V2660 | GSK-J4 | 1373423-53-0 | GSK J4 is a novel,cell permeable, and potent prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase (KDM) JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and is inactive against a panel of demethylases of the JMJ family. |
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V75860 | GSK-LSD1 | 1431368-48-7 | GSK-LSD1 is an LSD1 inhibitor. |
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V0376 | GSK-LSD1 2HCl | 1821798-25-7 | GSK-LSD1 2HCl, thedihydrochloride salt of GSK-LSD1 (GSK-LSD-1), is an irreversible, potent and selectiveinhibitor ofLysine (K) -specific demethylase 1A (LSD1) with antineoplastic activity. |
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V52029 | GSK-LSD1 dihydrochloride | 2102933-95-7 | GSK-LSD1 diHCl is a potent, selective, irreversible inhibitor of lysine-specific demethylase (LSD1) with IC50 of 16 nM. |
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V4128 | GSK2807 TFA | 2245255-66-5 | GSK2807 TFA (GSK-2807 TFA), the trifluoroacetic acid salt form ofGSK2807, is a selective and SAM-competitiveSMYD3inhibitorwith potential antitumor activity. |
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V3597 | GSK2879552 | 1401966-69-5 | GSK2879552 (GSK-2879552) is a novel, potent and orally bioavailable, irreversible inhibitor oflysine specific demethylase 1 (LSD1)with potential anticancer activity. |
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V52036 | GSK2879552 dihydrochloride | 1902123-72-1 | GSK2879552 diHCl is an orally bioavailable, irreversible LSD1/KDM1A inhibitor (antagonist) with anti-tumor activity. |
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V51995 | HDAC-IN-57 | 2716217-79-5 | HDAC-IN-57 is an orally bioactive pan-inhibitor of histone deacetylase (HDAC) with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6 and HDAC8 respectively. |
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V79995 | HDAC6-IN-3 | HDAC6-IN-3 (Compound 14) is an active anti-prostate cancer molecule and a potent, orally bioactive HDAC6 inhibitor (antagonist) with IC50 range of 0.02- 1.54 μM. | |
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V0374 | Iadademstat (ORY-1001; RG6016) 2HCl | 1431326-61-2 | Iadademstat (ORY-1001; RG6016) 2HCl, the dihydrochloride salt of ORY1001, is a novel, orally bioactive and selective lysine-specific demethylase LSD1/KDM1A inhibitor with antineoplastic activity. |
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V51948 | INCB059872 | 1802909-49-4 | INCB059872 is a potent, orally bioactive, selective and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. |
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V76894 | INCB059872 dihydrochloride | INCB059872 di-HCl is a potent, orally bioactive, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). | |
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V0372 | IOX1 | 5852-78-8 | IOX1 (5-Carboxy-8-hydroxyquinoline) is a novel, potent and broad-spectrum inhibitor of 2OG oxygenases (e. |
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V51922 | JHDM-IN-1 | 1310809-17-6 | JHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor (antagonist) with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM for JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively. |
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V0371 | JIB-04 (NSC-693627) | 199596-05-9 | JIB-04 (also known as NSC693627) is anovel, potent and pan-selective inhibitor of Jumonji histone demethylase (JMJD) inhibitor with antineoplastic activity. |
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V22899 | JIB-04 Z-isomer | 199596-24-2 | JIB-04 Z-isomer, formerly known as NSC 693627, is the Z-configurational isomer of JIB-04 whichis a potent and pan-selectiveJumonji histone demethylase inhibitor withIC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. |
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V54879 | JMJD3/HDAC-IN-1 | 2883046-06-6 | JMJD3/HDAC-IN-1 (compound A5b) is a dual (bifunctional) inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC50=16 nM). |
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V53409 | JMJD6-IN-1 | 899548-78-8 | JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor (antagonist) with 82% inhibition at 10 μM. |
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V51921 | JMJD7-IN-1 | 311316-96-8 | JMJD7-IN-1 is a potent JMJD7 inhibitor (antagonist) with IC50 of 6.62 μM. |
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