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 |
|---|---|---|---|---|
|
V56074 | (1R,2S)-NCD38 TFA | 2078047-42-2 | (1R,2S)-NCD38 TFA is an enantiomer of NCD38 TFA. |
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V52401 | Arborinine | 5489-57-6 | Arborinine is a potent orally bioactive LSD1 inhibitor. |
|
V2982 | AS8351 | 796-42-9 | AS8351 is a potent inhibitor of KDM5B (lysine-specific histone demethylase 5B) which plays an important role in maintaining cancer stem cells and justifies the rationale for studying the effects of continuous inhibition of this epigenetic factor in cancer. |
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V77191 | Bomedemstat dihydrochloride (IMG-7289 dihydrochloride) | Bomedemstat (IMG-7289) di-HCl is an orally bioactive and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). | |
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V56076 | CBB1003 hydrochloride | 2070015-02-8 | CBB1003 HCl is an inhibitor (blocker/antagonist) of histone demethylase LSD1 with IC50 of 10.54uM. |
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V17664 | CBB1007 | 1379573-92-8 | CBB1007 can penetrate cells and is a selective inhibitor of hLSD1 with IC50 of 5.27 μM. |
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V56067 | CBB1007 hydrochloride | 2070014-96-7 | CBB1007 HCl is a highly efficient substrate competitive, reversible, and selective inhibitor of the histone demethylase LSD1, with IC50 of 5.27 uM for hLSD1. |
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V52955 | CBB1007 trihydrochloride | 2070015-03-9 | CBB1007 triHCl is a selective inhibitor of LSD1 with IC50 of 5.27uM. |
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V75857 | cis-4-Br-2,5-F2-PCPA (S1024) | 2821068-03-3 | cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with a Ki of 94 nM and a Ki of 8.4 for LSD2 μM. |
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V2606 | CPI-455 | 1628208-23-0 | CPI-455 is a novel, potent andspecific inhibitor of the KDM5demethylase which catalyzes the demethylation of histone H3 on lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs). |
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V10836 | CPI-455 hydrochloride | 2095432-28-1 | CPI-455 HCl is a specific pan-KDM5 inhibitor (antagonist) with IC50 of 10 nM for KDM5A. |
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V2936 | DDP-38003 dihydrochloride | 1831167-98-6 | DDP-38003 dihydrochloride, atranylcypromine (TCPA) derivative, is a novel, potent and orally bioavailable inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1). |
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V77096 | DDP-38003 trihydrochloride | DDP-38003 triHCl is a novel, orally bioactive KDM1A/LSD1 inhibitor (antagonist) with IC50 of 84 nM. | |
|
V56182 | Eicosapentaenoic Acid-d5 (EPA-d5; Timnodonic acid-d5) | 1197205-73-4 | Eicosapentaenoic Acid-d5 is the deuterium labelled form of Eicosapentaenoic Acid. |
|
V21424 | Furazolidone | 67-45-8 | Furazolidone is a nitrofuran derivative with potent antiprotozoal and antibacterial activity. |
|
V80080 | FY-21 | FY-21 is a selective LSD1 inhibitor (IC50=340 nM) with antiproliferation and anti-colony-forming activities. | |
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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. |
|
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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