Biologically Active Small Molecules
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15(R)-HEDE
Cayman Chemical15(R)-HEDE is isolated by the chromatographic resolution of (±)15-HEDE. There are no reports of biological activity associated with 15(R)-HEDE in the literature.
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Fumonisin B1
Cayman ChemicalA mycotoxin produced from F. moniliforme that functions as an inhibitor of ceramide synthase (sphingosine N-acyltransferase).
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Bioymifi
Cayman ChemicalA DR5 agonist (Kd= 1.2 µM; IC50 = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.
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AZ 20
Cayman ChemicalA potent, selective inhibitor of ATR (IC50 = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.
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ARRY-162
LKT LabsARRY-162 is an orally bioavailable noncompetitive inhibitor of MEK1/2 and ERK that shows anticancer chemotherapeutic activity. Inhibition of MEK inhibits downstream signaling by IL-1, IL-6, and TNF. ARRY-162 inhibits proliferation in melanoma, non-small-cell lung cancer (NSCLC), head/neck cancer,…
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Thymoquinone
Cayman ChemicalA natural phytochemical with anti-inflammatory effects; inhibits the growth of leukemia cells (IC50 = 1.5 μg/ml), inducing apoptosis; at 15 μM, suppresses STAT3-regulated gene expression and prevents angiogenesis.
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Fura-2 AM
Cayman ChemicalAnoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma
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Aflatoxin G2
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.
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Mn(III)TMPyP
Cayman ChemicalMn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.
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Oclacitinib
Cayman ChemicalAn orally bioavailable, specific, broad spectrum JAK inhibitor (IC50s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and JAK4, respectively); blocks cell-based JAK signaling induced by IL-2, IL-4, IL-6, IL-13, or IL-31 with IC50 values ranging from 36 to 249 nM.
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Clodronate Disodium Tetrahydrate
LKT LabsClodronate is a first-generation non-nitrogen-containing bisphosphonate that is used clinically for its anti-resorptive activity. Clodronate generates formation of a non-hydrolysable ß-? ATP analog that inhibits mitochondrial ADP/ATP translocase and prevents mitochondrial oxygen consumption…
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Suberohydroxamic Acid
Cayman ChemicalA competitive HDAC inhibitor that inhibits HDAC1 (IC50 = 0.25 μM) and HDAC3 (IC50 = 0.30 μM); causes cell differentiation, cell cycle arrest, or apoptosis.
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Cdk5 Substrate
Cayman ChemicalA synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1; phosphorylated by Cdk5 with a Km value of 5 µM.
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Ochratoxin A
Cayman ChemicalA mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…
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Prostaglandin E2-d4-1-glyceryl ester
Cayman ChemicalAn internal standard for the quantification of PGE2-1-glyceryl ester by GC- or LC-MS.
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Canthaxanthin
LKT LabsCanthaxanthin is a carotenoid terpene pigment initially found in various sources including plants and fish. Canthaxanthin exhibits immunostimulatory, antioxidative, and chemopreventive activities; it does not display any vitamin A activity. In vivo, canthaxanthin increases cell-mediated and humoral…
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Benzyl Thiocyanate
LKT LabsChemopreventive. It inhibits cell proliferation in colorectal cancer cells and suppresses MAM acetate-induced carcinogenesis in vivo.
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Norgestimate
Cayman ChemicalA synthetic progestin that acts as a prodrug to norelgestromin and levonorgestrel; selectively binds the progesterone receptor and is androgenically neutral.
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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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4-hydroxy Nonenal Mercapturic Acid-d3
Cayman ChemicalAn internal standard for the quantification of 4-HNE mercapturic acid by GC- or LC-MS.
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Apixaban
Cayman ChemicalAn orally available, selective inhibitor of both free and prothrombinase-bound factor Xa (Ki = 0.8 nM); effective anticoagulant in both preclinical and clinical models of venous and arterial thrombosis.
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GDC-0152
Cayman ChemicalA potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.
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Cetirizine (hydrochloride)
Cayman ChemicalA second generation antihistamine that acts as a selective histamine H1 receptor antagonist (pKi = 8).
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a-Truxillic Acid
Cayman ChemicalCan be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.
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Montelukast (sodium salt)
Cayman ChemicalThe CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…
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Adenosine Kinase Inhibitor (hydrate)
Cayman ChemicalA non-nucleoside pyridopyrimidine compound that selectively blocks the action of adenosine kinase in an adenosine-competitive manner (IC50 = 1.7 nM in cell-free assays); suppresses nociception in various rodent pain models.
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Tyramine
Cayman ChemicalA trace amine that activates TAAR1 (EC50s = 0.08, 0.69, and 2.26 µM for rat, mouse, and human-rat chimera receptors, respectively); inhibits the release of norepinephrine and dopamine (IC50s = 40.6 and 119 nM, respectively).
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Olmesartan Medoxomil
Cayman ChemicalA prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.
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N-Oleoyl Glycine
Cayman ChemicalN-Oleoyl glycine is a putative substrate for peptidyl glycine α-amidating enzyme in the biosynthesis of oleoyl amide.
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GW 5074
Cayman ChemicalA potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM); blocks phosphorylation of ERK1/2 by 90% in cells stimulated with EGF when given at 5 µM; shows more than 100-fold selectivity for Raf-1 versus several related kinases.
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Isopropyl dodec-11-enylfluorophosphonate
Cayman ChemicalAn organophosphorus ester that antagonizes the CB1 receptor and inhibits FAAH with similar potencies (IC50s = 2 nM).