Biologically Active Small Molecules
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L-myo-Inositol-1,4,5-triphosphate (sodium salt)
Cayman ChemicalThe L isomer of the biologically important D-myo-inositol-1,4,5-triphosphate; does not evoke a rise in intracellular calcium when added to cells.
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OG-L002
Cayman ChemicalA potent inhibitor of LSD1 (IC50 = 0.02 µM) that less effectively inhibits MAO-A and MAO-B (IC50s = 1.38 and 0.72 µM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from…
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Elaiophylin
Cayman ChemicalA macrodiolide antibiotic that displays anti-protozoal activity against both Plasmodium and Trypanosoma (IC50s = 370 and 460 ng/ml, respectively) and cytotoxicity against MRC-5 cells (IC50 = 870 ng/ml); enhances the anti-fungal activity of rapamycin.
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Fluorescein-5-maleimide
Cayman ChemicalAn activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.
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17-AAG
Cayman ChemicalAn analog of geldanamycin which has potent in vivo activity and reduced toxicity; has diverse anti-tumor actions; promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC50 = 4-72 nM).
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Dexamethasone
Cayman ChemicalA synthetic glucocorticoid that binds the human glucocorticoid receptor with a higher affinity than a natural ligand, cortisol (Kd = 5 vs. 17 nM, respectively); has anti-inflammatory effects.
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XAV939
Cayman ChemicalA small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.
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Nitro Blue Tetrazolium (chloride)
Cayman ChemicalA chromogenic substrate that, like other tetrazolium compounds, can be reduced to produce a colored formazan derivative; used in the “NBT test” to evaluate the activity of NADPH oxidase in phagocytes; paired with PCIB for the colorimetric detection of alkaline phosphatase activity.
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7-keto Cholesterol
Cayman ChemicalA bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC50 = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.
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NADPH (sodium salt)
Cayman ChemicalThe reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.
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1,2-Dimyristoyl-sn-glycero-3-phosphate (sodium salt)
Cayman ChemicalA phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.
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Anastrozole
LKT LabsAnastrozole is a third generation aromatase inhibitor that suppresses synthesis of estrogen. Anastrozole exhibits anticancer chemotherapeutic activity and is clinically used to treat ER-positive breast cancer. In vitro, anastrozole inhibits proliferation of cancer cells by disrupting the…
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DBeQ
Cayman ChemicalA selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM); blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.
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CAY10429-d3
Cayman ChemicalAn internal standard for the quantification of CAY10429 by GC- or LC-MS.
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MMPIP (hydrochloride)
Cayman ChemicalA reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC50 = 26 nM).
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AZD 7545
Cayman ChemicalAn inhibitor of PDKs, resulting in an increase in PDH activity (EC50 = 5.2 nM for PDK2); less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).
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Colistin (sulfate)
Cayman ChemicalA polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.
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PF-8380
Cayman ChemicalA potent inhibitor of autotaxin (IC50 = 2.8 nM in an in vitro enzyme assay); at 30 mg/kg, reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).
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Guanosine 5'-triphosphate (sodium salt hydrate)
Cayman ChemicalA substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.
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1,2-Dimyristoyl-sn-glycero-3-PC
Cayman ChemicalA synthetic phosopholipid that can be used for liposome production in order to study the properties of lipid bilayers.
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Vitamin K3
Cayman ChemicalA precursor to Vitamin K2 that is capable of both redox cycling and arylating nucleophilic substrates by Michael addition; used as an antihemorrhagic agent and to inhibit the proliferation of various cancer cells.
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Golgicide A
Cayman ChemicalA reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC50 = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.
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GSA 10
Cayman ChemicalA SMO agonist that can promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM); used to characterize a novel SMO active site since it does not recognize the classic cyclopamine binding site utilized by other SMO agonists.
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N-Arachidonoyl-L-Serine
Cayman ChemicalAn endocannabinoid analog that does not bind to CB1, CB2, or TRPV1; at 5 mg/kg antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model; relaxes isolated rat mesenteric arteries and abdominal aorta, and increases the…
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Mecamylamine (hydrochloride)
Cayman ChemicalA noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC50 = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC50s range from 1-7 μM).
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CAY10571
Cayman ChemicalAn analog of SB203580, the highly specific pyridinylimidazole inhibitor of p38 MAPK; inhibits IL-1 production in the human monocytic cell line THP (IC50 = 0.20 µM) and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity (IC50 = 0.03 µM).
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Dihomo-y-Linolenic Acid ethyl ester
Cayman ChemicalDGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…
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GSK1059615
Cayman ChemicalA potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM) and the common activating mutants of p100α (E542K, E545K, and H1047R) found in cancer; prevents proliferation in BT474 tumor xenografts and reduces MAPK signaling with twice daily dosing at 25 mg/kg.
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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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PHA-767491
Cayman ChemicalAn inhibitor of Cdc7 kinase (IC50 = 10 nM) as well as Cdk9, (IC50 = 34 nM); induces apoptotic cell death in multiple cancer cell types at 10 µM.
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EW-7197
Cayman ChemicalEW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM). It also inhibits ALK2 and ALK4 at nanomolar concentrations. EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse…
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8-iso Prostaglandin F2ß
Cayman Chemical8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…