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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V80080 | FY-21 | FY-21 is a selective LSD1 inhibitor (IC50=340 nM) with antiproliferation and anti-colony-forming activities. | |
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V103459 | Geranylgeranoic acid | 35750-48-2 | Geranylgeranic acid (compound 5) inhibits lysine-specific demethylase 1 (LSD1) with an IC50 value of 46.97 µM. |
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V52030 | GSK 690 Hydrochloride | 2436760-79-9 | GSK 690 ( HCl) is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) with a Kd of 9 nM and IC50 of 37 nM. |
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V4761 | GSK J4 HCl | 1797983-09-5 | GSK J4 (GSK-J4) is a novel,cell permeable, and potent prodrug of GSK J1 with anti-inflammatory effects. |
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V3540 | GSK-690 | 2101305-84-2 | GSK 690 is a novel, potent and selective reversible inhibitor of lysine specific demethylase 1(LSD1), with aKdvalue of 9 nM and a biochemicalIC50of 37 nM. |
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V45816 | GSK-690 HCl | GSK-690 hydrochloride is a selective reversible inhibitor of lysine specific demethylase 1(LSD1) with anticancer activity. | |
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V76952 | GSK-J1 lithium salt | 2309668-29-7 | 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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V88877 | GSK-J1 sodium | 1797832-71-3 | GSK-J1 sodium is an 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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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 | 3023019-99-7 | 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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V96827 | HSP90/LSD1-IN-1 | HSP90/LSD1-IN-1 (Compound 6) is a dual HSP90/LSD1 inhibitor. | |
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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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V94282 | INCB059872 tosylate | 2081940-67-0 | INCB059872 mesylate is a potent, selective and orally active lysine demethylase 1 inhibitor. |