Endogenous Metabolite

Cat. No.

A73693

CAS No.

1851348-04-3

Pemetrexed tromethamine (dihydrochloric) dihydrate

Pemetrexed tromethamine (dihydrochloric) dihydrate is an endogenous metabolite targeting folate metabolism, primarily utilized as a chemotherapeutic agent. It exhibits potent anti-cancer activity, making it effective in the treatment of pleural mesothelioma and non-small cell lung cancer. This compound is instrumental in cancer research, particularly in studies focused on folate pathway inhibitors and their therapeutic implications.

Cat. No.

A73712

CAS No.

865451-66-7

R1663

R1663 is a selective inhibitor of factor Xa, demonstrating significant anticoagulant activity without affecting bleeding time. Its pharmacodynamic effects, such as the inhibition of thrombin generation, are dose-dependent, contributing to the prolongation of clotting time in a concentration-dependent manner. R1663 effectively reduces the peak height of thrombin generation and the endogenous thrombin potential, making it a valuable tool for research in coagulation and thrombus formation.

Cat. No.

A73773

CAS No.

175014-68-3

hCAI/II-IN-9

hCAI/II-IN-9 is a potent inhibitor of human carbonic anhydrase isoforms I, II, IX, and XII. It exhibits a range of inhibition constants (Ki) from 0.47 to 2.83 nM for hCA XII, indicating strong inhibitory activity, along with notable activity against hCA I, II, and IX. This compound has potential applications in the exploration of various pathologies associated with dysregulated carbonic anhydrase activity, making it valuable for research in cancer, glaucoma, and metabolic disorders.

Cat. No.

A73826

CAS No.

7296-30-2

Safrazine hydrochloride

Safrazine hydrochloride is a monoamine oxidase inhibitor (MAOI) known for its irreversible activity. By inhibiting monoamine oxidase, it effectively increases the levels of monoamine neurotransmitters, which plays a crucial role in alleviating symptoms of depression and mood disorders. This compound is valuable for research into the biochemical mechanisms underlying mood regulation and therapeutic approaches to mood disorders.

Cat. No.

A73830

CAS No.

1177460-72-8

Besigliptin tosylate

Synonyms: SHR117887

Besigliptin tosylate is a selective DPP-4 inhibitor that enhances metabolic control and β-cell function. It effectively lowers serum DPP-4 activity and improves oral glucose tolerance, demonstrating significant reductions in fasting blood glucose levels and enhanced lipid profiles in diabetic mouse models. Additionally, chronic administration of besigliptin tosylate increases insulin staining in pancreatic islet cells, underscoring its potential to improve β-cell function in therapeutic applications related to diabetes management.

Cat. No.

A73847

CAS No.

1781233-72-4

(Rac)-PAT-494

(Rac)-PAT-494 is a type II autotaxin inhibitor that specifically targets the enzyme responsible for the production of lysophosphatidic acid (LPA) in the bloodstream. By antagonizing autotaxin, (Rac)-PAT-494 exhibits promising potential in addressing diseases associated with cancer, fibrosis, and inflammation. It demonstrates high efficacy in biochemical assays and plasma tests, and has been shown to effectively lower plasma LPA levels following oral administration in rat models.

Cat. No.

A73862

CAS No.

1166398-85-1

Radamide

Radamide is a selective inhibitor of Grp94, targeting this chaperone protein to exhibit anti-migratory effects. It is primarily utilized in research related to Grp94-associated conditions, including glaucoma, cancer metastasis, and multiple myeloma. Additionally, Radamide derivatives have demonstrated enhanced potency and selectivity through optimized structure-activity relationship studies, making them valuable tools for investigating Grp94's role in various biological contexts.

Cat. No.

A73892

CAS No.

758722-12-2

AZD4877 hydrochloride

AZD4877 hydrochloride is a selective inhibitor of the microtubule motor protein kinesin-5 (KSP), primarily utilized for its anti-tumor properties. By inhibiting dynein's function, AZD4877 disrupts mitotic spindle assembly, activating the spindle assembly checkpoint and resulting in cell cycle arrest during mitosis. This disruption may lead to apoptosis in rapidly dividing cancer cells, while potentially reducing the risk of peripheral neuropathy commonly associated with other microtubule-targeted therapies. AZD4877 plays a critical role in ensuring the formation of bipolar spindles and the accurate segregation of sister chromatids during cell division.

Cat. No.

A73899

CAS No.

913636-88-1

H-0104 dihydrochloride

H-0104 dihydrochloride is a selective inhibitor of Rho-associated protein kinase (ROCK), targeting pathways involved in ocular pressure regulation. This compound has been shown to effectively lower intraocular pressure (IOP) in preclinical models, specifically in monkey eyes. It warrants further investigation to elucidate the mechanisms underlying its IOP-lowering effects, which may not solely rely on ROCK inhibition. H-0104 dihydrochloride is valuable for research applications focused on glaucoma and other conditions associated with elevated IOP.

Cat. No.

A73908

CAS No.

949164-80-1

NP603

NP603 is a potent inhibitor of Fibroblast Growth Factor Receptor 1 (FGFR1). It demonstrates significant anti-proliferative activity against endothelial cells, particularly in Human Umbilical Vein Endothelial Cells (HUVEC) stimulated by recombinant human FGF-2, with a minimum effective dose of 0.4 µM. This compound is valuable for research applications focused on angiogenesis and related signaling pathways.

Cat. No.

A73927

CAS No.

1781233-84-8

PAT-494

PAT-494 is an autotaxin (ATX) inhibitor that demonstrates significant anti-lyso-phosphatidic acid (LPA) activity in biochemical and plasma assays. This compound effectively reduces LPA levels in rat plasma upon oral administration, making it a valuable tool for studying LPA-related biological processes. Structural and activity studies have revealed a novel binding mode of PAT-494, allowing it to effectively occupy the hydrophobic pockets and channels of ATX, thereby providing insights into ATX modulation in various pathological conditions.

Cat. No.

A73938

CAS No.

56600-73-8

AKR1C2/3-IN-2

AKR1C2/3-IN-2 is a selective inhibitor targeting the aldo-keto reductase 1C3 (AKR1C3). This compound effectively inhibits AKR1C3-mediated production of testosterone and induction of prostate-specific antigen (PSA), thereby interfering with the endocrine functions of prostate cancer cells. Its selectivity for AKR1C3 over other aldo-keto reductases suggests its potential utility in addressing drug-resistant prostate cancer. Additionally, AKR1C2/3-IN-2 shows no inhibitory activity against cyclooxygenase (COX) isomerases, reinforcing its specificity in prostate cancer research applications.

Cat. No.

A73995

CAS No.

860385-36-0

Guanoxyfen nitrate

Synonyms: N-(3-Phenoxypropyl)guanidine nitrate; (3-Phenoxypropyl)guanidine nitrate

Guanoxyfen nitrate is a targeted inhibitor of the serine protease TMPRSS2, which is essential for the entry of coronaviruses into host cells. This compound exhibits significant biological activity by inhibiting TMPRSS2-mediated proteolytic processes, thereby diminishing viral infectivity. Additionally, guanoxyfen nitrate effectively suppresses vasoconstrictor responses to sympathetic nerve stimulation, making it a valuable reagent for research in virology and cardiovascular physiology.

Cat. No.

A74017

CAS No.

1227163-49-6

AZD-3289

AZD-3289 is a potent β-secretase 1 (BACE1) inhibitor, aimed at modulating the production of β-amyloid protein. Its primary biological activity involves reducing β-amyloid accumulation in the brain, which may contribute to slowing the progression of Alzheimer's disease. AZD-3289 is primarily utilized in research focused on neurodegenerative disorders, with potential applications in enhancing cognitive function by targeting the underlying mechanisms of Alzheimer's pathology.

Cat. No.

A74049

CAS No.

1206514-62-6

Demethyl PL265

Demethyl PL265 is a selective dual ENKephalinase inhibitor (DENKi) targeting the enzymatic breakdown of endogenous enkephalins. This compound demonstrates significant potential in alleviating pain through the modulation of endogenous opioid signaling pathways. Its ability to enhance enkephalin levels may provide valuable insights into pain management strategies and the study of opioid-related mechanisms in neurobiology.

Cat. No.

A74076

CAS No.

35301-24-7

Cedefingol

Cedefingol is an endogenous metabolite that acts as an α-glucosidase inhibitor. This compound demonstrates antitumor properties and exhibits diverse bioactivities influenced by the fermentation time of dark tea samples. Additionally, cedefingol displays antioxidant activity, as evidenced by its effectiveness in the DPPH assay. Research applications include studies on metabolic pathways, enzymatic processes, and potential therapeutic effects in cancer research.

Cat. No.

A74110

CAS No.

128253-12-3

hLTA4H/hLTA4S-IN-1

hLTA4H/hLTA4S-IN-1 is a dual inhibitor targeting human leukotriene hydrolase (hLTA4H) and human leukotriene C4 synthase (hLTC4S). This compound effectively disrupts the leukotriene biosynthesis pathway, making it valuable for studying inflammatory responses at the cellular level. hLTA4H/hLTA4S-IN-1 serves as a useful tool for research focused on leukotriene-related diseases and inflammatory conditions.

Cat. No.

A74115

CAS No.

77517-29-4

Dihydromevinolin

Synonyms: Lovastatin EP impurity E; 4a,5-Dihydromevinolin

Dihydromevinolin is a potent hypocholesterolemic metabolite derived from the fermentation of Aspergillus terreus. As an inhibitor of HMG-CoA reductase, it effectively reduces cholesterol biosynthesis. This compound is valuable for research applications focused on lipid metabolism and cholesterol regulation.

Cat. No.

A74122

CAS No.

1275996-50-3

KRP-109

KRP-109 is a potent inhibitor of neutrophil elastase (NE), demonstrating significant activity in mitigating lung inflammation. In mouse models, KRP-109 has been shown to enhance survival rates and decrease neutrophil accumulation within the alveolar walls. This compound effectively reduces cell and neutrophil counts in bronchoalveolar lavage fluid, as well as lowers levels of pro-inflammatory cytokines, including interleukin 1β and macrophage inflammatory protein 2. KRP-109 is valuable for research focused on severe pneumonia and associated inflammatory conditions.

Cat. No.

A74136

CAS No.

1332879-51-2

Pitstop 1

Pitstop 1 is a small molecule inhibitor that targets the endocytic pathway. It effectively disrupts the interaction between chaperones and the Krasin terminal domain, leading to altered Krasin functionality. This compound demonstrates potent biological activity by inhibiting Krasin-mediated signaling and is valuable in research applications focused on viral entry and pathogen interactions with host cells.

Cat. No.

A74142

CAS No.

1034474-19-5

MK-6186

MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor that demonstrates sub-nanomolar activity against wild-type viruses and common NNRTI-resistant RT mutants, including K103N and Y181C. This compound exhibits significant antiviral efficacy, particularly against K103N and Y181C mutant strains. When evaluated against 12 common NNRTI-associated mutant viruses, MK-6186 shows minimal resistance, with most viral strains demonstrating fold change values below 10. In clinical virus isolates harboring NNRTI-resistant mutations, a majority exhibit significantly reduced resistance to MK-6186 compared to other treatments. This positions MK-6186 as a promising candidate for research focused on combating NNRTI-resistant HIV strains.

Cat. No.

A74164

CAS No.

67273-56-7

NADH-IN-2

NADH-IN-2 is a potent inhibitor of Type II NADH dehydrogenase, an enzyme involved in the electron transport chain and cellular respiration. By selectively targeting this enzyme, NADH-IN-2 can modulate metabolic processes and influence energy production in cells. This compound is useful in research applications investigating bioenergetics, mitochondrial function, and metabolic disorders.

Cat. No.

A74176

CAS No.

897-83-6

Diethylumbelliferyl phosphate

Synonyms: DEUP

Diethylumbelliferyl phosphate (DEUP) acts as a selective and potent inhibitor of cholesterol esterase. This compound effectively disrupts steroidogenesis by inhibiting the transport of cholesterol into the mitochondria of steroidogenic cells, with an IC50 of 11.6 μM. DEUP is valuable in research applications focused on cholesterol metabolism and steroid hormone synthesis.

Cat. No.

A74179

CAS No.

3484-65-9

Aspergillomarasmine A

Aspergillomarasmine A is a natural aminopolycarboxylic acid that functions as an inhibitor of class B metallo-β-lactamases (MBLs). It specifically inactivates these enzymes by chelating the essential Zn2+ cofactor, effectively promoting the degradation of zinc-deficient NDM-1 and enhancing the efficacy of β-lactam antibiotics. This compound serves as a selective Zn2+ scavenger, demonstrating broad potential for research applications aimed at understanding and overcoming β-lactam resistance in bacterial pathogens.

Cat. No.

A74219

CAS No.

902502-82-3

ML262

ML262 is a potent inhibitor of hepatic lipid droplet formation, with an IC50 of 6.4 nM in murine AML-12 cells. This compound is significant in research related to non-alcoholic fatty liver disease, as it selectively targets lipid metabolism without inducing cytotoxicity at concentrations up to 33 μM. Additionally, ML262 does not interfere with fatty acid uptake at concentrations up to 50 μM, making it a valuable tool for studying lipid homeostasis and related metabolic disorders.