Metabolism

Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.

SDZ285428 is a CYP51 inhibitor.

Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM.

1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor.

NSC-703786 (5F-203) is a cytotoxic molecule that forms DNA adducts leading to cell death. NSC-703786 induces aryl hydrocarbon receptor signaling, and elevates expression of CYP1A1. Treatment of cells with NSC-703786 also leads to elevation of reactive oxygen species and activation of p38, JNK and ERK.

TM5007 is a poent inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 29 uM.

Tangshenoside I, isolated from the roots of Codonopsis lanceolata, exhibits weak α-glucosidase inhibitory activities in vitro with an IC50 of 1.4 mM.

Mitochondrial Ribosomal Protein L13 Human Recombinant

Mitochondrial RRNA Methyltransferase 1 Human Recombinant

Serine/Threonine Kinase 16, Mouse Anti Human

5',3'-Nucleotidase, Mitochondrial Human Recombinant

Serum/Glucocorticoid Regulated Kinase 1 Human Recombinant

Mitochondrial Trans-2-Enoyl-CoA Reductase Human Recombinant

Serine/Threonine Kinase 16 Human Recombinant

Serine/Threonine Kinase 17B Human Recombinant

Serine/Threonine Kinase 3 Human Recombinant

Serine/Threonine Kinase 17A Human Recombinant

3-Oxoacyl-ACP Synthase, Mitochondrial Human Recombinant

Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.

N-Acetyloxytocin is isolated and characterized in the neurointermediate lobe of the rat pituitary (NIL) and their presence in several brain areas of the rat.

γ-Glu-Gly, a γ-glutamyl dipeptide, is a human lipid metabolite.γ-Glu-Gly has a similar structure to GABA (γ-aminobutyric acid) and can act as an antagonist of excitatory amino acids.

Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase.

H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells.

Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.

Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α.

Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect.

Rimtoregtide is a polypeptide compound which significantly reduces the increase in the levels of amylase and lipase in the blood caused by acute pancreatitis. Rimtoregtide has the potential for the research of pancreatitis and acute pancreatitis (extracted from patent WO2018205233A1).

Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis.

Xenin is a 25-amino acid peptide initially isolated from human gastric mucosa. Xenin is a gut hormone that can reduce food intake.

Meldonium is a cardioprotective agent. It inhibits γ-butyrobetaine hydroxylase (BBOX) and carnitine/organic cation transporter type 2 (OCTN2).

Kifunensine is a potent and selective inhibitor of class I α-mannosidases, originally isolated from *Actinomycete* species. It blocks the trimming of mannose residues from N-linked glycoproteins by inhibiting α-mannosidase I activity, thereby preventing proper glycoprotein maturation. Through this mechanism, Kifunensine disrupts endoplasmic reticulum–associated degradation (ERAD) pathways, leading to the accumulation of misfolded glycoproteins. It is widely used as a biochemical tool in studies of protein folding, quality control, and glycosylation.

NNK is a tobacco-specific nitrosamine derived from nicotine and is a well-established carcinogenic compound. It activates both ERK1/2 and PKCα signaling pathways, leading to phosphorylation of Bcl-2 at Ser70 and c-Myc at Thr58 and Ser62, thereby promoting cell survival and proliferation in human lung cancer cells. Due to its strong tumorigenic potential, NNK is widely used to induce lung cancer in experimental mouse models for studying carcinogenesis and evaluating anticancer therapeutics.

Solasonine is a naturally occurring steroidal glycoalkaloid isolated from *Solanum melongena* (eggplant), known for its anti-infective, anticancer, and neurogenesis-promoting properties. It acts as a ferroptosis inducer by disrupting the glutathione redox system through inhibition of glutathione peroxidase 4 (GPX4). By promoting ferroptotic cell death in hepatocellular carcinoma (HCC) cells, Solasonine serves as a valuable compound for investigating ferroptosis mechanisms and developing novel anticancer strategies.

BODIPY 581/591 C11 is a boron-dipyrromethene (BODIPY) derivative with excellent photostability and minimal fluorescence artifacts. It is widely used to study lipid peroxidation and antioxidant activity in living cells, and to detect ferroptosis through its reaction with hydroxyl radicals. The dye exhibits a fluorescence shift upon oxidation: the reduced form emits at 591 nm (Ex: 581 nm), while the oxidized form emits at 510 nm (Ex: 500 nm).

Manumycin A is a polyketide antibiotic that functions as an inhibitor of thioredoxin reductase 1 (TrxR-1). It exhibits anti-tumor activity by inhibiting breast cancer cell growth, potentially through LC3-mediated mechanisms. Manumycin A also downregulates pro-inflammatory cytokine release in TNF-α-stimulated human monocytes, indicating anti-inflammatory potential. Additionally, it inhibits the Ras/Raf/ERK1/2 signaling pathway and hnRNP H1 in castration-resistant prostate cancer cells, thereby suppressing exosome biogenesis and secretion.

Pyridoxal 5′-phosphate monohydrate is the active coenzyme form of vitamin B6 and is essential for the function of numerous enzymes. It serves as a key cofactor for aromatic L-amino acid decarboxylase, which catalyzes the final step in the biosynthesis of the neurotransmitters dopamine and serotonin. Pyridoxal 5′-phosphate is the primary intracellular phosphorylated form of vitamin B6 and is interconvertible with other forms, including pyridoxine 5′-phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).

ZSH-2208 is a retinoic acid A analog that exhibits potent antitumor activity against tumor regenerative stem cells (TRCs) in esophageal squamous cell carcinoma (ESCC). Its mechanism of action involves the RARγ–TNFAIP3 signaling pathway.

ATP (Adenosine 5'-triphosphate) dimagnesium is a key molecule in cellular energy storage and metabolism. It supplies metabolic energy for ion pumps and other enzymatic processes and functions as a coenzyme in numerous cellular reactions. Additionally, ATP dimagnesium acts as an important endogenous signaling molecule involved in immune and inflammatory responses.

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of the translation of proprotein convertase subtilisin/kexin type 9 (PCSK9). It inhibits PCSK9 expression by inducing ribosomal stalling at approximately codon 34 during translation.

BRD4/NAMPT-IN-1 (Compound A2) is a dual inhibitor of NAMPT and BRD4, with IC₅₀ values of 35 nM and 58 nM, respectively. It suppresses the growth and migration of hepatocellular carcinoma cells and induces apoptosis. In the HCCLM3 xenograft mouse model, BRD4/NAMPT-IN-1 exhibits potent anticancer activity without apparent toxicity.

Ganodermanontriol, a sterol isolated from *Ganoderma lucidum*, exerts anti-inflammatory effects in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells by upregulating heme oxygenase-1 (HO-1) expression. It demonstrates hepatoprotective activity.

5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases, including mammalian 5-C-MTase, and binds to DNA in a manner dependent on DNA stem-loop structure formation. It directs de novo DNA methylation by serving as a methylation mark, promoting methylation of adjacent CpG sites in single-stranded DNA via cis-acting mechanisms. 5mdC regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, influencing chromatin condensation and gene expression. In plant cells, its distribution correlates with cell proliferation and differentiation stages, with lower methylation levels in proliferating cells and higher levels in differentiated cells.

NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor with an IC₅₀ of 1.2 μM. It selectively binds to residues within the NNMT substrate-binding site. NNMTi promotes myoblast differentiation in vitro and enhances the fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice, making it a promising compound for research into muscle regeneration and age-related muscle decline.

Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.

Triolein is a symmetric triacylglycerol composed of three oleic acid molecules esterified to glycerol. It exhibits strong antioxidant and anti-inflammatory properties and has been shown to reduce the upregulation of matrix metalloproteinase-1 (MMP-1), a key enzyme involved in tissue remodeling and inflammation. These activities make triolein a compound of interest in research related to inflammatory diseases and oxidative stress.

Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties.

Tin protoporphyrin IX dichloride (SnPPIX) is a potent inhibitor of heme oxygenase-1 (HO-1), an enzyme involved in cellular stress responses and tumor progression. SnPPIX has been shown to sensitize pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mouse models, enhancing therapeutic efficacy and supporting its potential use as a chemosensitizing agent in cancer treatment.

HET0016 is a potent and selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthase, with IC50 values of 17.7 nM, 12.1 nM, and 20.6 nM for CYP4A1-, CYP4A2-, and CYP4A3-mediated 20-HETE synthesis, respectively. It also acts as a selective cytochrome P450 (CYP450) inhibitor and has been shown to suppress angiogenesis and tumor growth, making it a valuable compound for cancer and vascular research.

Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is a broad-spectrum antibiotic with demonstrated efficacy against *Mycoplasma bovis*, exhibiting a MIC₉₀ of 0.312 μg/mL. In addition to its antibacterial properties, it also shows inhibitory activity against vaccinia virus (VV), indicating potential antiviral applications.

C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability.