dna methylation

Dihydro-5-azacytidine FA (DHAC) is a pyrimidine analog that has antitumor activity, inhibits cell growth, inhibits DNA methylation, and may be used in the study of malignant mesothelioma.

5-Methyl-2'-deoxycytidine (5MedCyd) is a pyrimidine nucleoside that when incorporated into single-stranded DNA can act in cis to signal de novo.

Caffeic acid is a dual inhibitor of 5-lipoxygenase and TRPV1 ion channels.

Streptozotocin (Streptozocin, NSC-85998) is an antibiotic that enters pancreatic β-cells via the glucose transporter (GLUT2) and induces DNA methylation, leading to β-cell apoptosis. It is toxic to insulin-producing cells and commonly used to establish diabetic animal models. This product is unstable in solution and is recommended to be prepared freshly before use.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

Uracil is a common naturally occurring pyrimidine found in RNA, it base pairs with adenine and is replaced by thymine in DNA. Methylation of uracil produces thymine. Uracil's use in the body is to help carry out the synthesis of many enzymes necessary for cell function through bonding with riboses and phosphates. Uracil serves as allosteric regulator and coenzyme for many important biochemical reactions.

5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity.

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

Hydralazine hydrochloride (Apresoline) is the hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume, and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells.

Zebularine (4-Deoxyuridine) is a DNA methylation inhibitor. Acts as a transition state analog inhibitor of cytidine deaminase by binding to the active size as covalent hydrates. It also inhibits cytidine deaminase (Ki: 2 μM, in a cell-free assay).

7-Methylguanine is an orally available PARP1 inhibitor (Ki=61 μM) that competes with the substrate NAD+, exhibiting anticancer activity. As a natural nucleic acid metabolite, it may serve as a probe for protein-DNA interactions.

VAL-083 is an alkylating agent with antitumor activity that produces N7 methylation on DNA.

Anhydroleucovorin is the predominant, biologically active form of vitamin B9 (folate) that is utilized by the body for a multitude of vital cellular functions, including DNA synthesis, repair, and methylation, as well as the production of key neurotransmitters; Anhydroleucovorin plays an essential metabolic role in the remethylation pathway, converting the amino acid homocysteine to methionine, and serves as the main folate form found in systemic circulation and transported into tissues for physiological use.

S-adenosylmethionine is a precursor of taurine and cysteine, acting through methylation, sulphuration, and peptide synthesis. It promotes the formation of the MetJ-DNA complex, a transcription repressor of methionine in E. coli.

Ryuvidine is a dual inhibitor of KDM5A and SETD8, an inducer of the DNA damage response with potential anticancer activity, inhibition of H4K20 methylation, and inhibition of CDK4, and can be used to study breast cancer and erythroplasia.

Ademetionine (S-adenosylmethionine; SAMe) is a ubiquitous metabolite present in all cells and biological fluids, and serves as a methyl donor in a multitude of different methylation reactions involving proteins, phospholipids, catecholamines and DNA.

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032, a first-in-class, non-time-dependent, non-covalent, reversible, selective DNMT1 inhibitor with an IC50 of 0.036 μM, which induces robust loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth.

HPV18-IN-1 (Compound H1) is a potent HPV18 inhibitor that prevents premature cell progression and abnormal proliferation in cervical cancer cells. By suppressing the E7-Rb-E2F cellular pathway and DNA methylation, HPV18-IN-1 holds potential for cancer research.

LX-3 is a selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway, which de-represses a subset of endogenous genes repressed by DNA methylation.

LX-5 is a selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway. LX-5 de-represses a subset of endogenous genes repressed by DNA methylation.

LX-4 is a selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway. LX-4 de-represses a subset of endogenous genes repressed by DNA methylation.

S-Adenosyl-L-methionine iodide is a universal methyl donor in vivo, participating in the methylation of DNA, RNA, and proteins, playing a core role in gene regulation and cellular homeostasis.

Dihydro-5-azacytidine acetate (DHAC), a nucleoside analog, integrates into DNA to inhibit DNA methylation and exhibits antitumor activity [1] [2].

Methyl 3,4-dimethoxycinnamate impedes uredospore germination and concurrently inhibits global DNA methylation in Hep3B cells [1] [2].