Biologically Active Small Molecules
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R-848
Cayman ChemicalAn immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.
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ß-Cembrenediol
LKT LabsCembrenediols are diterpenes originally found in Anisomeles. These compounds exhibit antibacterial activity against Mycobacterium and antifungal activity against Colletotrichum. Grade: ≥98%
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2-Chloroadenosine
Cayman ChemicalA metabolically stable adenosine analog that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively; anticonvulsive activity in a rat model of generalized seizures.
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Aflatoxin B2
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin B2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.
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Aflatoxin G1
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G1 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.
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Cefoperazone Acid
LKT LabsCefoperazone is a third generation β-lactam cephalosporin antibiotic. Cefoperazone exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding proteins to prevent peptidoglycan synthesis and bacterial cell wall formation. Cefoperazone also…
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NS3694
Cayman ChemicalA cell-permeable diarylurea compound that inhibits apoptosome formation and caspase activation; blocks cytochrome c-induced caspase activation in HeLa cell cytosolic extracts with an IC50 value of approximately 50 µM; suppresses caspase activation and apoptosis in cells treated…
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Nobiletin
Cayman ChemicalA natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC50 = 11.5 and 4.9 μM, respectively).
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RQ-00203078
Cayman ChemicalA selective TRPM8 antagonist (IC50s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
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Chenodeoxycholic Acid
LKT LabsChenodeoxycholic acid is an endogenous bile acid synthesized by the liver; it acts as an agonist at the farnesoid X receptor (FXR). Chenodeoxycholic acid exhibits anticancer and gastrointestinal motility modulating activities. This compound treats chronic constipation and displays protective…
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Ceftriaxone Sodium
LKT LabsCeftriaxone is a third generation β-lactam cephalosporin antibiotic. Ceftriaxone exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding protein activity to prevent peptidoglycan synthesis and bacterial cell wall formation. Ceftriaxone is…
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Doxazosin (mesylate)
Cayman ChemicalA non-selective α-adrenergic receptor antagonist with pKi values of 8.5, 9, and 8.4 for human α1A, α1B, and α1D adrenoceptors, respectively; used to relax smooth muscles of the prostate in clinical studies designed to examine treatments that improve lower urinary tract…
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LLP-3
Cayman ChemicalA cell-permeable ligand of Survivin that blocks its interaction with Ran, resulting in the induction of apoptosis in glioma stem cells (IC50 = 31 µM); abolishes the growth of glioblastoma multiforme cell in spheres and in tumor slice cultures.
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PF-04620110
Cayman ChemicalA potent and selective inhibitor of DGAT-1 (IC50 = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.
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CAY10657
Cayman ChemicalA thiophene carboximide derivative proposed to inhibit IKK2; likely to be useful in the treatment of inflammatory diseases and cancer.
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Arachidonoyl Cyclopropylamide
Cayman ChemicalA potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…
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Bis(3,5-dibromosalicyl) Fumarate
LKT LabsBis(3,5-dibromosalicyl) fumarate is an aspirin analog that is used to induce hemoglobin chain crosslinks at lysine residues. This compound is used to study hemoglobin function in research models and may be used to develop treatments for sickle-cell anemia. This compound may exhibit…
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JNJ-26854165
Cayman ChemicalAn antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways.
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2,7-Dichlorodihydrofluorescein diacetate
Cayman ChemicalA fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.
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5-Iodotubercidin
Cayman ChemicalInitiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).
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ML-099
Cayman ChemicalA small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.
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Citrinin
LKT LabsCitrinin is a mycotoxin initially produced by Penicillum, Aspergillus, and Monascus. Citrinin exhibits cytotoxic, cardiotoxic, nephrotoxic, and pro-oxidative activities. In leydig cells, citrinin inhibits testosterone production and induces caspase-mediated apoptosis. In embryos, citrinin alters…
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CYM 5442
Cayman ChemicalA selective SIP1 agonist (EC50 = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC50 = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.
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Camostat (mesylate)
Cayman ChemicalA trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.
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Ezatiostat
Cayman ChemicalA tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM); restores JNK-mediated cellular proliferation and differentiation signaling pathways.
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CYM 5541
Cayman ChemicalA selective agonist of S1P3 (EC50 = 72-132 nM); less effectively activates S1P1 (EC50 = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.
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Allicin
LKT LabsAllicin is an thiocyanate found in garlic; it exhibits a wide variety of properties, including anticancer, antioxidative, antihypertensive, anti-arrhythmic, anti-parasitic, and anti-diabetic activities. In vitro, allicin binds cellular nucleic acid, primarily nitrogenous bases and phosphate…
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Acivicin
Cayman ChemicalA glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively); reversibly inhibits γ-glutamyl transpeptidase.
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Genipin
Cayman ChemicalA protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…
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17-trifluoromethylphenyl-13,14-dihydro trinor Prostaglandin F2a
Cayman ChemicalA number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma. Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.…
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Acridine Orange
Cayman ChemicalA cell-permeable, fluorescent dye that accumulates in acidic organelles in a pH-dependent manner and is used for autophagy detection and cell cycle determination; emits green fluorescence (ex. max: 502 nm; ,em. max: 525 nm) at neutral pH or when bound to dsDNA and red fluorescence (ex. max: 460 nm;…
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