cancer metabolism

DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Emitefur (BOF-A 2) is an orally active and potent 5-fluorouracil derivative with anticancer and antitumor activity.Emitefur is used in advanced gastric cancer, breast cancer and metabolism-related diseases.

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A/B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

5-Fluorouridine is a metabolite of 5-fluorouracil that inhibits rRNA synthesis in human colon cancer cells and exhibits antitumor and antiviral activity. 5-Fluorouridine exerts a cytotoxic effect on the growth of L1210 cells, with an IC₅₀ value of 2 nM. 5-Fluorouridine binds to poly-A RNA and exhibits antiproliferative activity. 5-Fluorouridine can be used in studies of nucleic acid metabolism, cancer chemotherapy, and viral replication mechanisms.

Liquiritin (Liquiritigenin-4'-O-glucoside) (LIQ) is a main component among the licorice flavonoids, and possesses anti-inflammatory and anti-cancer abilities.

D-Fructose-1,6-bisphosphate sodium salt hydrate is the intermediate in carbohydrate metabolism, including glycolysis and gluconeogenesis. During glycolysis, it is produced by phosphorylation of fructose-6-phosphate by phosphofructokinase. The reverse reaction mediated by fructose-1, 6-diphosphatase-1 is one of the rate-limiting steps of gluconeogenesis. The same reaction occurs in the chloroplasts of plants, D-Fructose-1,6-bisphosphate sodium salt hydrate as part of the reducing pentose phosphate cycle. Since cancer cells use glycolysis as a primary source of metabolic energy production, this pathway has become a major target for cancer chemotherapy.

Cyclocreatine, a creatine analogue and substrate for creatine kinase, inhibits creatine metabolism and prostate cancer cell proliferation, improving cognitive, autistic and epileptic phenotypes in mouse models of creatine transporter deficiency (CTD).

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

DX3-234 is a potent oxidative phosphorylation (OXPHOS) inhibitor that acts by inhibiting complex I in the mitochondrial electron transport chain (ETC), leading to intracellular ATP depletion and cell death, and can be used for the treatment of specific cancers dependent on aerobic metabolism, such as pancreatic cancer.

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor with nanomolar-level inhibitory effects on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP production, leading to impaired cellular energy metabolism and cancer cytotoxicity.

SIRT5 inhibitor 5 is a selective and substrate-competitive SIRT5 inhibitor with an IC50 of 210 nM, which does not occupy the NAD+ binding pocket and can be used to study cancer and metabolism-related diseases.

LCL521 dihydrochloride is a dual inhibitor of acid ceramidase (ACDase) and lysosomal acid sphingomyelinase (ASMase). By targeting these lysosomal enzymes, LCL521 dihydrochloride modulates sphingolipid metabolism, with potential applications in cancer and metabolic disorder research.

Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction of apoptosis in melanoma cells.

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).

FX-11 (LDHA Inhibitor FX11) is a highly potent, selective, and competitive inhibitor of lactate dehydrogenase A (LDHA), with a Ki value of 8 μM for LDHA. FX-11 acts as an activator of PKM2 (pyruvate kinase M2). FX-11 exerts its antitumor effects by inhibiting glycolysis, depleting ATP, and inducing oxidative stress and apoptosis. FX-11 can be used in tumor metabolism research.

HFI-142 is a small-molecule inhibitor that binds specifically to the active site of aminopeptidase N and suppresses its enzymatic activity. HFI-142 has been demonstrated to inhibit leukotriene A4 biosynthesis in red blood cells, an effect that may offer therapeutic potential for the research in cancer by modulating inflammatory and metabolic pathways implicated in tumor growth and progression. HFI-142 was also shown to inhibit the activity of additional aminopeptidases, including aminopeptidase N, as well as other enzymes associated with protein metabolism.

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta

1-Methyladenosine-D3 is the hydrochloride salt form of deuterium-labeled 1-Methyladenosine. This compound is a modification of RNA that serves as a biomarker for tumors, with elevated levels in the body linked to cancer development. Upon methylation, 1-Methyladenosine (T7571) upregulates the expression of PPARδ, regulates cholesterol metabolism, and activates the Hedgehog signaling pathway, thereby driving the onset of liver tumors.