demethylation

Epoxiconazole (BAS-480F) is a 14-α demethylase inhibitor. It inhibits ergosterol synthesis and fungal cell wall formation.

Hexademethylation Schisandrin A is a natural product that can be used in related research in the field of life sciences. Its product number is TN8812.

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

Myclobutanil (Systhane) is a triazole chemical used as a fungicide. It is a steroid demethylation inhibitor, specifically inhibiting ergosterol biosynthesis. Ergosterol is a critical component of fungal cell membranes.

Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor with an IC50 of 151 nM. Entacapone is also a potential obesity-related gene (FTO) inhibitor that can inhibit FTO demethylation activity and be used in the study of metabolic diseases.

Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM, respectively.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

Hexaconazole ((-)-Hexaconazol) is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death.

Sulconazole mononitrate (Exelderm) is the nitrate salt form of sulconazole, a synthetic imidazole derivative with the antifungal property. Sulconazole mononitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and inhibition of the synthesis of ergosterol, an important component of the fungal cell membrane. Inhibition of ergosterol synthesis leads to a disruption of cell membrane permeability, and ultimately inhibition of cell wall synthesis. In addition, Sulconazole mononitrate seems to interfere with the autolytic degradation of fungal DNA and RNA.

Flutriafol is a pesticide, demethylation inhibitor, and NMDA receptor agonist

LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes. LY 43578 can be used to study neurological and cardiovascular diseases.

1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.

Thalifendine is one of the main products of Berberine demethylation catalyzed by CYP51 (secreted by intestinal flora), which has anti-inflammatory effects, reduces intestinal inflammation, improves intestinal barrier function, and reduces the production of inflammatory factors.

Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Likely inhibiting cytochrome P450-dependent demethylation of lanosterol, it prevents ergosterol synthesis, a crucial component of the fungal cell membrane. This disruption of membrane synthesis and integrity alters permeability, promotes loss of essential intracellular components, and inhibits fungal cell growth.

LSD1-IN-35 (Compound Z-1) is a selective inhibitor of LSD1, exhibiting an IC50 of 108 nM. This compound inhibits the demethylation of H3K4me1/2 and acts as an immunomodulator. Additionally, LSD1-IN-35 enhances the responsiveness of gastric cancer cells to T-cell killing by reducing PD-L1 expression, thereby weakening the PD-1/PD-L1 interaction.

193 D7 is an orally bioavailable and selective JMJD1C inhibitor with an IC₅₀ of 0.59 μM and a Kd of 1.96 μM. In HTRF assays, it blocks the binding of JMJD1C to the H3K9me2 peptide substrate with an IC₅₀ of 1.47 μM. 193 D7 regulates the fitness of regulatory T cells (Tregs) in the tumor microenvironment via a dual mechanism: it promotes H3K9me2 enrichment to downregulate PD-1 expression and inhibits STAT3 demethylation to enhance STAT3 activation. It exhibits dose-dependent antitumor activity in multiple mouse tumor models, including MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatoma, and CT26 colorectal cancer, and can be used as a tool molecule for selectively targeting intratumoral Tregs in tumor immunity research.

PROTACKDM4 degrader-1 (Compound 11) is a proteolysis-targeting chimera (PROTAC) degrader specifically designed for KDM4. It effectively degrades KDM4A-C while sparing KDM4D. In esophageal cancer cells, PROTACKDM4 degrader-1 demonstrates strong antiproliferative activity, inducing apoptosis and cell cycle arrest, and inhibits lysine demethylation of histone H3.

AW4 is an LSD1 inhibitor. In demethylation assays involving H3K4me2, AW4 suppresses the activity of LSD1 ΔTTAS. AW4 is applicable for research on drug resistance.

Arasertaconazole, a sterol-14-alpha demethylation inhibitor, is used potentially for the treatment of vulvovaginal candcanidiasis.

Bitertanol (KWG 0599) is a triazole fungicide. Bitertanol inhibits demethylation, disrupts membrane function, and prevents sterol synthesis.

5-formylcytosine (5FC) is a rare base found in mammalian DNA. It participates in active DNA demethylation, changes DNA double helix structure, and reduces the transcription rate and substrate specificity of RNA polymerase II.

Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

HM-cytosine (5hmC) is a naturally occurring component of mammalian genomic DNA and is thought to be the sixth base of DNA [1]. HM-cytosine is an intermediate metabolite for demethylation of active DNA [2]. HM-cytosine is an ep

N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS)Anal. Bioanal. Chem.402(3)1217-1227(2012) 2.Bai, X., Wang, X.P., He, G.D., et al.Simultaneous determination of rosuvastatin, rosuvastatin-5 S-lactone, and N-desmethyl rosuvastatin in human plasma by UPLC-MS/MS and its application to clinical studyDrug Res. (Stuttg.)68(6)328-334(2018)