Biologically Active Small Molecules, 1 mg, UN2811
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ML-354
Cayman ChemicalA PAR4 antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.
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Cucurbitacin B
Cayman ChemicalA plant-derived steroidal triterpene that induces cell cycle arrest or apoptosis in a range of cancer cell lines; inhibits the growth of several breast cancer cell lines (IC50s = 18-50 nM); suppresses the growth of tumors developed from MDA-MB-231 and 4T-1 breast cancer cells in mice.
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Fusarenon X
Cayman ChemicalA type B trichothecene mycotoxin found in cereals contaminated with certain Fusarium species.
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1-hydroxy Vitamin D2
Cayman ChemicalA synthetic prodrug of 1,25-dihydroxy vitamin D2; used to suppress the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; stimulates bone growth; inhibits the growth of certain blastomas and prostate cancer cells.
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(-)-Warfarin
Cayman ChemicalAn anticoagulant; differs from (+)-warfarin by being five times more potent as a vitamin K antagonist; has a shorter terminal elimination half-life (24-33 hours) than (+)-warfarin (35-58 hours).
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Clozapine N-oxide
Cayman ChemicalA major metabolite of clozapine; used in designer receptor exclusively activated by designer drug, also known as DREADD, technology to modulate synthetic receptors in vivo.
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L-779,450
Cayman ChemicalAn ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that inhibits cell proliferation both in B-Raf mutated and wild-type melanoma cell lines.
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UK 383367
Cayman ChemicalA potent, selective inhibitor of BMP1 (IC50 = 44 nM); effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.
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10074-G5
Cayman ChemicalA c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM); cytotoxic to c-Myc-overexpressing cells lines (IC50s = 15.6 and…
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Cucurbitacin I
Cayman ChemicalA potent inhibitor of the STAT3/JAK signaling pathway; suppresses levels of tyrosine phosphorylated STAT3, STAT3 DNA binding and STAT3-mediated gene transcription; suppresses tumor growth in vivo.
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Cytochalasin E
Cayman ChemicalInhibits actin polymerization; potently and selectively inhibits the growth of endothelial cells (IC50 1 protease activity.
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Chetomin
Cayman ChemicalA natural product which acts as a small molecule inhibitor of HIF signaling, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations; effectively attenuates the HIF pathway both in cells and in vivo, in mice.
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1,25-dihydroxy Vitamin D2
Cayman ChemicalThe active circulating metabolite of vitamin D2 formed by 25-hydroxylase in the liver and 25-hydroxyvitamin D-hydroxylase in the kidney.
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Gambogic Acid
Cayman ChemicalAn anti-cancer natural product that acts on a variety of cellular pathways; activates caspases, inhibits anti-apoptotic proteins, alters expression of Bcl-2 and Bax; acts as a potent, slow inhibitor of Kir2.1 channels; inhibits the chymotrypsin activity of the 20S proteasome; has effects on AMPK,…
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Citreoviridin
Cayman ChemicalA mycotoxin that inhibits the mitochondrial ATP synthetase system; inhibits soluble ATPase (KD = 4.1 µM), ADP-stimulated respiration in isolated rat liver mitochondria (KD = 0.15 µM), and ATP-driven reduction of NAD+ by succinate (KD = 2 µM).
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(±)-Verapamil-d3 (hydrochloride)
Cayman ChemicalAn internal standard for the quantification of verapamil (hydrochloride) by GC- or LC-MS.
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Thapsigargin
Cayman ChemicalA non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM); increases intracellular calcium, leading to cell activation, histamine release, and increased cell proliferation; has anti-inflammatory and anti-cancer effects…
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Epothilone B
Cayman ChemicalA macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…
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Moniliformin (sodium salt)
Cayman ChemicalA mycotoxin produced by fungi of the Fusarium genus that is phytotoxic to various agriculture grain crops, cardiotoxic to poultry and rats, and cytotoxic to human red blood cell progenitors (IC50 = 4.1 μM).
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3-Acetyldeoxy Nivalenol
Cayman ChemicalA trichothecene mycotoxin that can be converted to DON in the body.
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Apicidin
Cayman ChemicalA fungal toxin that demonstrates selective inhibition of HDAC3/NcoR over HDAC6 (IC50s = 15.8 and 665.1 nM, respectively); has broad spectrum activity against Apicomplexan parasites and exhibits antiproliferative activity against various cancer cell lines (IC50s = 0.13-2.36 μM).
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Prostaglandin E1 Alcohol
Cayman ChemicalA non-irritant bronchodilator with relaxant activity on human bronchial muscle; binds to the mouse recombinant EP3 and EP4 receptors with Ki values of 330 and 190 nM, respectively.
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6-keto Prostaglandin E1
Cayman Chemical6-keto PGE1 is a metabolite isolated after the incubation of PGI2 with rabbit liver microsomes. However, it is not produced in appreciable amounts following IV infusion of PGI2 in humans. 6-keto PGE1 is equipotent with PGI2 as a vasodilator; in most other aspects its activity resembles PGE1.
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Cevimeline (hydrochloride)
Cayman ChemicalA muscarinic receptor agonist (EC50s = 23, 48, and 63 nM for M1, M3, and M5, respectively, and >1 µM for M2 and M4); stimulates secretion by salivary glands and is useful in ameliorating xerostomia (dry mouth).
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Tenuazonic Acid
Cayman ChemicalA major Alternaria mycotoxins commonly found as a food contaminant (LD50 = 548 μg/egg in the chicken embryo toxicity assay) and linked to esophageal cancer in human populations at risk of high exposure; Mice fed 100 mg/kg/day orally for 10 months developed precancerous lesions on the esophageal mucosa.
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Oxytocin
Cayman ChemicalA nonapeptide hormone primarily synthesized in the hypothalamus with roles in uterine contraction and lactation, social memory and attachment, sexual and maternal behavior, aggression, learning, anxiety, feeding, and pain perception.
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Phallacidin
Cayman ChemicalA natural mycotoxin that binds F-actin; contains a carboxyl group for coupling reactions.
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Fumonisin B2
Cayman ChemicalA mycotoxin from F. moniliforme, a fungus of grains; at 1 μM, inhibits sphingosine N-acyltransferase; fumonisins, found as contaminants in foods, induce apoptosis via altered sphingolipid metabolism, resulting in hepatotoxicity and nephrotoxicity.
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25-hydroxy Vitamin D3
Cayman ChemicalAn intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.