s-adenosylmethionine

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.

FIDAS-3, a stilbene derivative and potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A), exhibits anticancer activities by effectively competing with S-adenosylmethionine (SAM) for MAT2A binding.

FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. It can effectively compete with S-adenosylmethionine for MAT2A binding and has anticancer effects.

S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.

Sardomozide dihydrochloride (CGP 48664 dihydrochloride) is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC, IC50 = 5 nM).

S-Adenosyl-L-methionine disulfate tosylate is a methyl donor with oral activity. S-Adenosyl-L-methionine disulfate tosylate is a dietary supplement with effective antidepressant and pain-relieving effects. S-Adenosyl-L-methionine disulfate tosylate also has anti-proliferative, pro-apoptotic and anti-metastatic effects in cancer. S-Adenosyl-L-methionine can be used in the research of liver diseases and osteoarthritis.

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

Mitoguazone (Methyl-GAG) is a selective S-adenosyl-methionine decarboxylase inhibitor that penetrates the blood-brain barrier and disrupts polyamine biosynthesis. Mitoguazone is a synthetic polycarbonyl derivative with anti-tumor activity that inhibits the integration of HIV DNA into cellular DNA in monocytes and macrophages, inducing apoptosis. Mitoguazone can be used to prevent acute leukemia, Hodgkin lymphoma and non-Hodgkin lymphoma.

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.

S-Adenosyl-L-methionine (SAMe) 1,4-butanedisulfonate functions as an orally active methyl group donor and serves as a dietary supplement known for its significant antidepressant properties. Additionally, it plays anti-proliferative, pro-apoptotic, and anti-metastatic roles in cancer. SAMe 1,4-butanedisulfonate holds promise in research pertaining to cancer, liver disease, and osteoarthritis [1] [2] [3].

S-Adenosyl-L-methionine (S-Adenosyl methionine) chloride dihydrochloride functions as a methyl donor and cofactor.

AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A) that penetrates the blood-brain barrier. It inhibits S-adenosylmethionine (SAM) metabolizing enzymes and MAT2A for the treatment of cancer and for studying the role of SAM regulation in the central nervous system (CNS).

Sardomozide is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC)(IC50 of 5 nM).

AGI-41998 tautomers is a tautomerism of pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]-. pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]- is a S-adenosylmethionine synthase isoform type-2 inhibitor, IC50= 0.022μM.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

(S)-Tubercidinylhomocysteine (Page 46) is a potent inhibitor of S-adenosylmethionine-dependent methyltransferases. It is useful in studies of herpes viruses (HSV) and vaccinia virus (VV).

SARS-CoV-2 nsp14-IN-10 is a highly effective and selective inhibitor of the NSP14 (IC50 = 0.34 µM) S-adenosylmethionine (SAM) binding pocket. This compound exhibits significant antiviral activity against SARS-CoV-2 and has broad-spectrum efficacy against other β-coronaviruses. It inhibits the replication phase of SARS-CoV-2 and also suppresses viral translation while stimulating immune responses. Additionally, SARS-CoV-2 nsp14-IN-10 can specifically reverse NSP14-mediated alterations in the host transcriptome. It is a valuable compound for research on SARS-CoV-2.

S-Aristeromycinylhomocysteine is an inhibitor of adenosylmethionine decarboxylase.

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.

S-Farnesyl thioacetic acid, an analog of S-farnesyl cysteine, acts as a competitive inhibitor of isoprenylated protein methyltransferase (S-adenosylmethionine-dependent methyltransferase) and inhibits the methylation of both farnesylated and geranylgeranylated substrates.

N-acetyl-S-geranylgeranyl-L-Cysteine is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

CGP 40215 is a specific S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor that was found to inhibit the growth of Leishmania donovani promastigotes

MDL-73811 is a potent AdoMetDC (S-adenosylmethionine decarboxylease) inhibitor and anti-trypanosomal compound that cures Brucella infections in mice. However despite the good activity of MDL 73811, rapid plasma clearance and poor brain penetration hindered its further development.

SARS-CoV-2-IN-60 (compound 5a) is a specific, irreversible inhibitor of SARS-CoV-2 nsp16-nsp10 methyltransferase, competing with S-adenosylmethionine (SAM) and exhibiting an IC50 of 9 µM and a Ki of 26 µM. It binds to a novel pocket near the SAM-binding site on nsp16, suggesting potential as a pan-coronavirus therapeutic [1].