Biologically Active Small Molecules
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Primary Prostaglandin Metabolite LC-MS Mixture
Cayman ChemicalContains selected eicosanoids produced by the metabolism of prostaglandins; designed for direct use in LC-MS applications.
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Linolein Hydroperoxides
Cayman ChemicalLinolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…
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Altretamine
LKT LabsAltretamine is an anticancer chemotherapeutic agent that binds DNA at guanine and cytosine residues, forming DNA adducts. This alkylating agent is also metabolized to formaldehyde. Altretamine is clinically used to treat ovarian cancer.
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AZD 1080
Cayman ChemicalA potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist MK-801.
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Nitrendipine
Cayman ChemicalA dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A1, A2A, and A3 receptors with Ki values of 8.96, 23.0, and 8.3 µM, respectively.
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trans-Resveratrol-3-O-ß-D-Glucuronide
Cayman ChemicalA regioisomeric resveratrol metabolite that may be used as a reference standard for accurate determination of the metabolic profile of resveratrol.
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Pseurotin A
Cayman ChemicalA secondary metabolite produced by fungi; inhibits IgE production by mouse B cells in culture (IC50 = 3.6 μM) and dose-dependently (0.4-25 μg/ml) stimulates neuritogenic activity in rat pheochromocytoma PC12 cells; demonstrates nematicidal activity at 300 μg/ml.
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5(Z),11(Z),14(Z)-Eicosatrienoic Acid
Cayman Chemical5(Z),11(Z),14(Z)-Eicosatrienoic acid is a PUFA found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was…
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ML-204
Cayman ChemicalML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…
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Carbenoxolone Disodium
LKT LabsCarbenoxolone is a synthetic derivative of glycyrrhizin that exhibits anti-ulcerative, anti-inflammatory, neuromodulatory, neuroprotective, anti-hyperlipidemic, hepatoprotective, and immunosuppressive activities. Carbenoxolone is clinically used to treat ulcers and inflammation; it inhibits…
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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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Myricetin
Cayman ChemicalA flavonoid compound that acts as a powerful antioxidant; inhibits TBARS formation with an IC50 value of 6.34 µM; blocks oxLDL uptake by U937-derived macrophages at 20 µM; demonstrates potent chemopreventative potential by binding JAK1/STAT3 to inhibit neoplastic transformation of…
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O-Acetyl Salicylhydroxamic Acid
Cayman ChemicalO-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a…
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L-Mimosine
Cayman ChemicalA non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC50 = 3.7 µM).
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Palmitic Acid
Cayman ChemicalA common 16-carbon saturated fatty acid that represents 10-20% of the normal human dietary fat intake.
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Colcemid
Cayman ChemicalA colchicine derivative that inhibits tubulin polymerization (IC50 = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.
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Nourseothricin (sulfate)
Cayman ChemicalA broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.
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ISCK03
Cayman ChemicalA cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.
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GNF-5
Cayman ChemicalA selective allosteric inhibitor of Bcr-Abl (IC50s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…
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ONX 0914
Cayman ChemicalA selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse…
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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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DMOG
Cayman ChemicalA cell permeable, competitive inhibitor of HIF-1α prolyl hydroxylase; stabilizes HIF-1α expression at normal oxygen tensions in cultured cells at concentrations between 0.1 and 1 mM.
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Oleoyl Ethanolamide-d4
Cayman ChemicalAn internal standard for the quantification of OEA by GC- or LC-MS.
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Eggmanone
Cayman ChemicalA selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation.
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[Des-Asp1]-Angiotensin I, Human
LKT LabsAngiotensin I (AT I) is a peptide cleavage product of angiotensin and serves no primary biological purpose other than to function as a precursor to angiotensin II.
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Fulvestrant
Cayman ChemicalA potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.
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DC4 Crosslinker
Cayman ChemicalA MS-cleavable crosslinking reagent (18Å in length) that contains two intrinsic positive charges, which allow cross-linked peptides to fragment into their component peptides by collision-induced dissociation or in-source decay.
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Fatty Acid ethyl ester Standard Pack
Cayman ChemicalThe Fatty Acid ethyl ester Standard pack contains a series of nine fatty acid ethyl esters. Each pack contains 100 mg of the ethyl esters of the following fatty acids: stearic, myristic, linoleic, linolenic, arachidonic, oleic, palmitic, lauric, and palmitoleic.
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(±)13(14)-EpDPA
Cayman ChemicalA DHA epoxygenase metabolite found in rat brain and spinal cord that acts as a preferred substrate for sEH (Km = 3.2 µM); demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models and potently inhibits angiogenesis and tumor growth in in vitro assays.
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BCATc Inhibitor 2
Cayman ChemicalA sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…
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CPI-613
Cayman ChemicalA lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.