Endogenous Metabolite

Cat. No.

A73301

CAS No.

303196-31-8

R1498

R1498 is a multi-target kinase inhibitor primarily affecting Aurora kinases and VEGFR2, associated with tumorigenesis. This compound exhibits notable anti-angiogenic and anti-proliferative properties, demonstrating moderate in vitro growth inhibition across various tumor cell lines with IC50 values in the micromolar range. In vivo studies reveal that R1498 surpasses sorafenib in anti-tumor efficacy within gastric cancer and hepatocellular carcinoma xenograft models, achieving tumor growth inhibition rates exceeding 80% along with substantial tumor shrinkage in select models. Additionally, R1498 effectively inhibits Aurora A activity and reduces tumor vascularization, underscoring its potential as a therapeutic candidate in oncology research.

Cat. No.

A73309

CAS No.

1060478-12-7

H2-005

H2-005 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2), effectively reducing triacylglycerol synthesis in both hepatocytes and preadipocytes. This compound demonstrates significant inhibition of triacylglycerol biosynthesis in HepG2 hepatocytes and 3T3-L1 preadipocytes. Additionally, H2-005 substantially inhibits lipid droplet formation in 3T3-L1 cells when used in conjunction with a DGAT1 inhibitor. This reagent is valuable for research related to DGAT2-mediated lipid metabolism and potential therapeutic strategies for metabolic disorders.

Cat. No.

A73311

CAS No.

247131-79-9

JTV-803 mesylate

JTV-803 mesylate is a selective inhibitor of human factor Xa, functioning as an oral anticoagulant. It demonstrates competitive inhibition with a Ki value of 0.019 μM and an IC50 value of 0.081 μM, showcasing a remarkable specificity over comparable inhibitors. JTV-803 is primarily used in research focused on thrombosis prevention and the modulation of coagulation pathways, making it a valuable tool for studies in cardiovascular and hematological contexts.

Cat. No.

A73318

CAS No.

81872-09-5

Zofenoprilat arginine

Zofenoprilat arginine is an endogenous metabolite that functions as an antihypertensive agent, primarily through the enhancement of bradykinin effects on coronary flow. This compound is of particular interest in cardiovascular research, especially in studies involving the interplay of sulfhydryl-containing converting enzyme inhibitors and bradykinin-mediated vasodilation. Its role in influencing vascular response makes it a valuable tool for understanding hypertension and related cardiovascular conditions.

Cat. No.

A73326

CAS No.

38455-99-1

BuChE-IN-14

BuChE-IN-14 is a selective inhibitor of acetylcholinesterase (AChE), primarily targeting endogenous metabolite pathways. In vitro studies demonstrated a concentration-dependent inhibition of AChE activity in rat brain tissue, leading to increased extracellular acetylcholine (ACh) levels in the hippocampus and striatum. This compound shows potential for addressing memory impairments linked to cholinergic dysfunction, making it valuable for research into neurodegenerative diseases and cognitive enhancement.

Cat. No.

A73346

CAS No.

207403-36-9

MR-16728 hydrochloride

MR-16728 hydrochloride is an endogenous metabolite that primarily promotes the release of acetylcholine through inhibition of Ca(2+)-ATPase activity in presynaptic membranes. It effectively enhances acetylcholine release and demonstrates significant activity in the presence of low calcium concentrations. Research applications include studying neurotransmitter release mechanisms and analyzing acetylcholine dynamics under various physiological conditions. The compound shows a half-maximal effect at a concentration of 13.5 μM, making it a valuable tool for investigating synaptic transmission and neuromodulation.

Cat. No.

A73369

CAS No.

2001072-35-9

DC_YM21

DC_YM21 is an inhibitor of the menin-MLL interaction, demonstrating potent and selective activity in blocking cellular proliferation. This compound effectively induces cell cycle arrest and promotes differentiation in leukemia cells with MLL translocations. DC_YM21 holds significant potential for research applications targeting MLL-rearranged leukemia treatments.

Cat. No.

A73454

CAS No.

616884-64-1

OMDM-3

OMDM-3 is a selective inhibitor of anandamide cellular uptake (ACU), exhibiting a Ki value of 16.6 μM. This compound is metabolically stable, making it suitable for studies investigating the role of anandamide in cannabinoid signaling and endocannabinoid system modulation. OMDM-3 can be utilized in research applications focused on pain management, neuroprotection, and the exploration of lipid signaling pathways.

Cat. No.

A73455

CAS No.

937051-40-6

DF 461

DF 461 is a selective sterol synthase inhibitor that effectively impairs cholesterol biosynthesis. Demonstrating high specificity for liver tissue, DF 461 significantly reduces cholesterol synthesis in rat liver models. This compound has also been shown to lower plasma lipid levels in repeated dosing studies in non-rodent species, making it valuable for research applications related to lipid metabolism and cardiovascular health.

Cat. No.

A73466

CAS No.

128201-92-3

IST-622

Synonyms: 6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin

IST-622 is an endogenous metabolite exhibiting significant anti-tumor activity through the inhibition of cancer cell growth. It demonstrates potent growth inhibitory effects against various mouse tumor models, including P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, and Colon 26 and 38 adenocarcinomas. Additionally, IST-622 is effective in human tumor xenograft models, notably large cell lung carcinoma and gastric adenocarcinoma. In vitro studies reveal an IC50 for P388 leukemia that is over 20 times lower than conventional treatments, underscoring its potential as a therapeutic agent in oncology research.

Cat. No.

A73468

CAS No.

2183470-13-3

GCN2iB acetate

GCN2iB acetate is a selective inhibitor of the GCN2 kinase, primarily targeting the Gcn2 signaling pathway. It enhances the phosphorylation of eIF2, leading to increased expression of Atf4, particularly in Gcn2 mutants with specific alterations in regulatory regions or kinase domain substitutions. This compound is valuable for studying cellular responses to nutritional stress and has potential applications in cancer research, specifically in sensitizing cancer cells with low levels of aspartate synthetase to the anti-leukemic agent L-aspartase.

Cat. No.

A73472

CAS No.

1200127-66-7

GNE-783

GNE-783 is a selective checkpoint kinase 1 (CHK1) inhibitor that plays a pivotal role in modulating the cell cycle response to DNA damage. By inactivating S-phase and G2-phase checkpoints, it enhances the efficacy of anti-metabolite chemotherapeutics, such as gemcitabine and temozolomide, particularly in melanoma cell lines. GNE-783 is instrumental in research applications focused on overcoming drug resistance and improving treatment outcomes across various tumor types.

Cat. No.

A73473

CAS No.

17968-82-0

Prostaglandin D1

Synonyms: PGD1

Prostaglandin D1 is an endogenous metabolite known for its role as a prostanoid. It exhibits both contractile and relaxant effects on isolated human pial arteries and acts as an inhibitor of ADP-induced platelet aggregation, with an IC50 value of 320 ng/ml. This compound is useful for studies in metabolic research and vascular biology.

Cat. No.

A73521

CAS No.

116457-99-9

Thioetheramide-PC

Synonyms: 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine

Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a modified phospholipid that serves as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). With an IC50 value of 2 μM at a substrate concentration of 0.5 mM, Thioetheramide-PC interacts with both the catalytic and activation sites of the enzyme, exhibiting tighter binding to the activation site. This unique dual interaction may facilitate phospholipase activation at low concentrations, making Thioetheramide-PC a valuable tool for studying sPLA2-related biological processes and mechanisms.

Cat. No.

A73545

CAS No.

251356-32-8

SU9518

SU9518 is a selective tyrosine kinase inhibitor targeting PDGFRα, demonstrating significant anti-fibrotic properties. This compound effectively inhibits the progression of proliferative vitreoretinopathy (PVR) in rabbit models involving fibroblasts and Müller cells, showing promising results without discernible toxicity. SU9518 holds potential for therapeutic applications in PVR and other proliferative ocular disorders characterized by fibrosis and gliosis.

Cat. No.

A73548

CAS No.

1604034-71-0

PF-05387252

PF-05387252 is a potent and selective inhibitor of IRAK4, effectively targeting endogenous Toll-like receptor (TLR) signaling pathways. This compound exhibits significant anti-inflammatory activity in experimental models, suggesting potential therapeutic applications in conditions such as psoriasis. While PF-05387252 has demonstrated efficacy in reducing inflammation in animal studies, its effectiveness in clinical settings for psoriasis has yet to be established.

Cat. No.

A73554

CAS No.

365462-24-4

Darexaban maleate

Synonyms: YM150 maleate

Darexaban maleate is a direct factor Xa inhibitor, primarily utilized in the research of venous thromboembolism prevention. Its major metabolite, Darexaban glucitol, exhibits pharmacological activity and is formed in the human liver and intestine via UGT1A9 and UGT1A10-mediated glucitolation. The glucitolation exhibits a K(m) value greater than 250 μM in the liver, while in the intestine, it displays substrate inhibition kinetics with a K(m) of 27.3 μM. The presence of fatty acid-free bovine serum albumin significantly lowers the unbound K(m) values in human liver microsomes and UGT1A9.

Cat. No.

A73575

CAS No.

1190196-77-0

PMPMEase-IN-2

PMPMEase-IN-2 is an inhibitor of polyprenylated protein methylesterase, targeting the regulation of polyprenylated protein metabolism. This regulation is crucial for maintaining normal cellular function and survival, with dysregulation linked to degenerative diseases and cancer. PMPMEase-IN-2 holds potential applications in cancer research, providing a specific approach for investigating the modulation of polyprenylated protein pathways.

Cat. No.

A73586

CAS No.

1883803-09-5

sEH-IN-12

sEH-IN-12 is a potent inhibitor of soluble epoxide hydrolase (sEH) that effectively blocks its activity. This compound demonstrates strong biological activity and has been utilized in the construction and selection of small molecule libraries. The development of sEH-IN-12 offers a valuable tool for drug discovery efforts aimed at targeting sEH for therapeutic interventions.

Cat. No.

A73650

CAS No.

1820763-99-2

BCM-599

BCM-599 is an endogenous metabolite that functions as a hepatitis B virus (HBV) capsid assembly inhibitor. It demonstrates potent antiviral activity with an IC50 value of 0.88 μM and a CC50 value of 144 μM in HepG2.2.15 cells. When administered in conjunction with lamivudine, BCM-599 exhibits a synergistic effect, enhancing the reduction of viral concentration. This compound is a valuable tool for investigating combined strategies for the treatment of HBV infection.

Cat. No.

A73655

CAS No.

261505-81-1

Sabiporide mesylate

Synonyms: BIIB 722 mesylate

Sabiporide mesylate is a selective inhibitor of sodium-hydrogen exchange, primarily targeting NHE1. This compound exhibits cardioprotective properties, rendering it an important reagent for studies on myocardial ischemia and myocardial infarction. Its ability to modulate sodium and hydrogen ion transport makes it useful in exploring cellular mechanisms linked to cardiac stress responses.

Cat. No.

A73665

CAS No.

893556-15-5

AZD-6605

AZD-6605 is a potent, reversible inhibitor targeting matrix metalloproteinases MMP2, MMP9, MMP12, and MMP13, exhibiting high selectivity. This compound was optimized for enhanced activity, solubility, and drug metabolism and pharmacokinetics (DMPK) properties by modifying the zinc hydroxide binding group found in traditional inhibitors. AZD-6605 is valuable for investigating the roles of these metalloproteinases in various biological processes and disease states, making it suitable for research applications in inflammation, cancer, and tissue remodeling studies.

Cat. No.

A73670

CAS No.

117978-26-4

A-62198

A-62198 is a selective renin inhibitor that exhibits significant antihypertensive properties. It effectively reduces mean arterial pressure (MAP) in anesthetized, salt-deprived primate models in a dose-dependent manner. Notably, A-62198 also demonstrates a statistically significant decrease in plasma renin activity (PRA) across all administered doses, making it a valuable tool for research in cardiovascular pharmacology and hypertension studies.

Cat. No.

A73674

CAS No.

908813-78-5

NSC-84096

NSC-84096 is an endopeptidase activity inhibitor that effectively inhibits the enzymatic activity of botulinum neurotoxin type A light chain (rBoNT/A-LC). Its ability to block this neurotoxin in vitro suggests a significant potential for use in research focused on botulism and related neurotoxic disorders. The mechanism of action for NSC-84096 may facilitate the development of small molecule therapeutics targeting these hazardous toxins.

Cat. No.

A73677

CAS No.

20535-76-6

p18SMI-21

p18SMI-21 is an innovative inhibitor targeting the INK4C protein, effectively blocking the biological activity of p18. This compound exhibits a significant reduction in the proteolytic activity of pepsin, demonstrating its potential as an anti-gastric acid agent. Its inhibitory efficacy is notably influenced by dosing and requires direct contact with the substrate to maintain its effect. p18SMI-21 is valuable for researchers investigating gastric acid dynamics and the regulatory mechanisms of p18 in cellular metabolism.