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one-carbon metabolism

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By Targets:	Amino Acid Derivatives (1) Apoptosis (1) Bcl-2 Family (1) Caspase (1) Cytochrome P450 (1) DNA/RNA Synthesis (1) Endogenous Metabolite (3) GABA Receptor (1) iGluR (1) Methylenetetrahydrofolate Dehydrogenase (MTHFD) (3) Reactive Oxygen Species (ROS) (2) SHMT (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (1) Infection (1) Metabolic Disease (1) Neurological Disease (3)

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Peptides

Natural
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Targets Recommended: Mitochondrial Metabolism

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0504

Creatinine 5+ Cited Publications NSC13123	Endogenous Metabolite GABA Receptor iGluR	Infection Neurological Disease Metabolic Disease Cancer
Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-113110

Cysteinylglycine L-Cysteinylglycine; Cys-Gly; H-Cys-Gly-OH	Endogenous Metabolite Reactive Oxygen Species (ROS) DNA/RNA Synthesis	Cardiovascular Disease Cancer
Cysteinylglycine (L-Cysteinylglycine; Cys-Gly) is a dipeptide formed by the peptide bond linkage between cysteine (Cysteine) and glycine (Glycine). Cysteinylglycine is an important metabolic intermediate in the human body, mainly derived from the degradation of glutathione (GSH). Cysteinylglycine reduces ferric iron to ferrous iron, drives the redox cycle of iron, generates reactive oxygen species (ROS), stimulates oxidative reactions, induces lipid peroxidation of human plasma LDL lipoproteins, and causes oxidative damage to DNA bases. Cysteinylglycine can be used as a biomarker to evaluate ischemic heart disease, breast cancer and other conditions .

HY-131943

DS44960156	Methylenetetrahydrofolate Dehydrogenase (MTHFD)	Neurological Disease Cancer
DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC₅₀=1.6 μM, K_i=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD ⁺/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers .

HY-162353

AZ'9567		Cancer
AZ'9567 is an orally active MAT2a inhibitor with a pIC₅₀ of 9.1. AZ'9567 binds to MAT2a allosterically, reduces the synthesis of SAM, decreases SDMA levels, and exerts antiproliferative effects on MTAP-knockout cells. AZ'9567 depletes SAM, causes methionine accumulation in plasma and tissues, triggers adaptive disorders in one-carbon metabolism, transsulfuration metabolism and lipid metabolism, and induces oxidative stress, hepatic steatosis and lipid homeostasis imbalance. AZ'9567 can be used in studies related to MTAP-deficient/deleted cancers .

HY-137829

5-Methyltetrahydrofolic acid disodium 5+ Cited Publications	Endogenous Metabolite	Others
5-Methyltetrahydrofolic acid disodium is the metabolite of Folinic acid (Leucovorin) (HY-17556). 5-Methyltetrahydrofolic acid disodium is involved in one-carbon metabolism and the transfer of methyl groups .

HY-182356

MTHFD1/2-IN-1	Methylenetetrahydrofolate Dehydrogenase (MTHFD)	Cancer
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC₅₀ values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .

HY-N18390

5-Methyltetrahydropteroyltri-L-glutamate	Amino Acid Derivatives	Neurological Disease Cancer
5-Methyltetrahydropteroyltri-L-glutamate is an amino acid derivative. 5-Methyltetrahydropteroyltri-L-glutamate is present in the dried extract of Allium sativum (Hisar Garlic No. 17). 5-Methyltetrahydropteroyltri-L-glutamate participates in the remethylation of homocysteine to methionine via cobalamin-independent methionine synthase. 5-Methyltetrahydropteroyltri-L-glutamate is a biomarker associated with altered one-carbon transfer reactions in glioblastoma. 5-Methyltetrahydropteroyltri-L-glutamate can be used in glioblastoma-related research .

HY-182284

Anticancer agent 310	Reactive Oxygen Species (ROS) Apoptosis Bcl-2 Family Caspase SHMT Methylenetetrahydrofolate Dehydrogenase (MTHFD) Cytochrome P450	Cancer
Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP ⁺ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer .

Cat. No.	Product Name	Target	Research Area

HY-113110

Cysteinylglycine L-Cysteinylglycine; Cys-Gly; H-Cys-Gly-OH	Endogenous Metabolite Reactive Oxygen Species (ROS) DNA/RNA Synthesis	Cardiovascular Disease Cancer
Cysteinylglycine (L-Cysteinylglycine; Cys-Gly) is a dipeptide formed by the peptide bond linkage between cysteine (Cysteine) and glycine (Glycine). Cysteinylglycine is an important metabolic intermediate in the human body, mainly derived from the degradation of glutathione (GSH). Cysteinylglycine reduces ferric iron to ferrous iron, drives the redox cycle of iron, generates reactive oxygen species (ROS), stimulates oxidative reactions, induces lipid peroxidation of human plasma LDL lipoproteins, and causes oxidative damage to DNA bases. Cysteinylglycine can be used as a biomarker to evaluate ischemic heart disease, breast cancer and other conditions .

Creatinine 5+ Cited Publications NSC13123	Infection Structural Classification Natural Products Classification of Application Fields Disease markers Endocrine diseases Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite GABA Receptor iGluR
Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

Cysteinylglycine L-Cysteinylglycine; Cys-Gly; H-Cys-Gly-OH	Natural Products Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite Reactive Oxygen Species (ROS) DNA/RNA Synthesis
Cysteinylglycine (L-Cysteinylglycine; Cys-Gly) is a dipeptide formed by the peptide bond linkage between cysteine (Cysteine) and glycine (Glycine). Cysteinylglycine is an important metabolic intermediate in the human body, mainly derived from the degradation of glutathione (GSH). Cysteinylglycine reduces ferric iron to ferrous iron, drives the redox cycle of iron, generates reactive oxygen species (ROS), stimulates oxidative reactions, induces lipid peroxidation of human plasma LDL lipoproteins, and causes oxidative damage to DNA bases. Cysteinylglycine can be used as a biomarker to evaluate ischemic heart disease, breast cancer and other conditions .

5-Methyltetrahydropteroyltri-L-glutamate	Structural Classification Alkaloids Other Alkaloids Allium sativum L. Euphorbiaceae Plants Acalypha indica Linn. Amaryllidaceae Source Classification	Amino Acid Derivatives
5-Methyltetrahydropteroyltri-L-glutamate is an amino acid derivative. 5-Methyltetrahydropteroyltri-L-glutamate is present in the dried extract of Allium sativum (Hisar Garlic No. 17). 5-Methyltetrahydropteroyltri-L-glutamate participates in the remethylation of homocysteine to methionine via cobalamin-independent methionine synthase. 5-Methyltetrahydropteroyltri-L-glutamate is a biomarker associated with altered one-carbon transfer reactions in glioblastoma. 5-Methyltetrahydropteroyltri-L-glutamate can be used in glioblastoma-related research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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one-carbon metabolism

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