Cayman Chemical Biologically Active Small Molecules
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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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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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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.
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trans-Resveratrol-d4
Cayman ChemicalAn internal standard for the quantification of trans-resveratrol by GC- or LC-MS.
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8-hydroxy Guanine (hydrochloride)
Cayman Chemical8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.
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Amlodipine
Cayman ChemicalA dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC50 = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…
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3,3'-Diindolylmethane
Cayman ChemicalPhytochemical from cruciferous vegetables that demonstrates anticancer and chemopreventative effects (10-30 µM) involving the induction of Phase 2 enzymes, promotion of apoptosis, induction of cell cycle arrest, inhibition of cell proliferation, and inhibition of histone deacetylases and DNA…
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PtdIns-(5)-P1 (1,2-dioctanoyl) (ammonium salt)
Cayman ChemicalA synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.
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Ketoconazole
Cayman ChemicalAn orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC50 = 63.5 nM), as well as a variety of other CYP isoforms.
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ZD 7288
Cayman ChemicalA potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC50s = 32 and 158 nM, respectively); modulates the sinoatrial node and slows heart rate; reduces neuropathic pain in several animal models.