Biologically Active Small Molecules, Cayman Chemical, 5 mg
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2-O-ethyl PAF C-16
Cayman Chemical2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…
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D-Mannoheptulose
Cayman ChemicalA heptose that inhibits glucokinases and hexokinases from diverse organisms through competition with D-glucose (Ki = 0.25 mM); blocks glucose oxidation and glucose-mediated insulin release from pancreatic islet cells.
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DL-Glyceraldehyde-3-phosphate
Cayman ChemicalAn intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.
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1-Deoxymannojirimycin (hydrochloride)
Cayman ChemicalA specific inhibitor of class I α-1,2-mannosidase (IC50 = 20 mM), a key enzyme for N-glycan processing in the endoplasmic reticulum and Golgi; inhibiting α-1,2-mannosidase with 1-Deoxymannojirimycin generates N-linked oligosaccharides with high mannose content, preventing…
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Hydroxy Linoleins
Cayman ChemicalHydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…
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CeMMEC1
Cayman ChemicalA selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC50 = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.
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Beraprost (sodium salt)
Cayman ChemicalBeraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…
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m-3M3FBS
Cayman ChemicalAn activator of PLC that stimulates superoxide generation, increase in cytoplasmic calcium, and inositol phosphate formation in human neutrophils when used at a concentration of 15-50 µM; promotes the hydrolysis of phosphatidylinositol bisphosphate by all PLC isoforms.
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(±)-C75
Cayman ChemicalA stable inhibitor of FAS that leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.
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Piriprost (potassium salt)
Cayman ChemicalPiriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC50 value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…
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SNS-032
Cayman ChemicalA selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC50 values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC90 value of 0.3 µM.
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1,2,3,4,6-Penta-O-galloyl-ß-D-glucopyranose
Cayman ChemicalA major component of the root of P. suffruiticosa that at 30 µM inhibits the growth of human hepatocellular carcinoma SK-HEP-1 cells by causing cell cycle arrest and suppressing the activation of NF-κB.
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Bicyclo Prostaglandin E2
Cayman ChemicalBicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…
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Epacadostat
Cayman ChemicalA selective IDO1 inhibitor (IC50 = 7.1 nM in HeLa cells); promotes T and natural killer-cell growth, increases IFN-γ production, and reduces conversion to Treg-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells; inhibits…
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E-64
Cayman ChemicalA natural, potent and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively; also inhibits papain, calpain, and cathepsins B and H.
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ML-030
Cayman ChemicalA triazolothiadiazine that inhibits PDE4 (EC50 = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC50 = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC50 = 48.2, 37.2, 452, and 49.2 nM, respectively).
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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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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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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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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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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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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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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.