Cayman Chemical, 5 mg, Biologically Active Small Molecules
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Crizotinib
Cayman ChemicalA potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC50 = 8 nM) and ALK (IC50 = 20 nM) receptor tyrosine kinases; shows antitumor efficacy in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins…
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Cobimetinib
Cayman ChemicalA selective, orally available inhibitor of MEK1 (IC50 = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.
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AH 6809
Cayman ChemicalAH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809 blocks the PGE2-induced accumulation of cAMP in COS cells transfected with the human EP2 receptor. It also blocks the accumulation of Ca2+ in Xenopus oocytes…
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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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Oleoyl Serotonin-d17
Cayman ChemicalAn internal standard for the quantification of oleoyl serotonin by GC- or LC-MS.
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Ginsenoside Rg2
Cayman ChemicalA protopanaxatriol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-diabetic actions; protects against DNA damage and apoptosis induced by ultraviolet light.
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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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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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CFTR Inhibitor-172
Cayman ChemicalA thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance.
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K252c
Cayman ChemicalK252c is a cell-permeable PKC inhibitor (IC50s = 2.45 and 25.7 µM for PKC and PKA, respectively). It induces apoptosis in human chronic myelogenous leukemia cancer cells. In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains…
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R-568
Cayman ChemicalA calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.
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C-6 NBD Ceramide
Cayman ChemicalC-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…
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11ß-Prostaglandin E2
Cayman Chemical11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…
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trans-ISRIB
Cayman ChemicalA symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC50 = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.
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13,14-dihydro-15-keto Prostaglandin F1a
Cayman Chemical13,14-dihydro-15-keto PGF1α is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.
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Quin-2 (potassium salt)
Cayman ChemicalA high-affinity fluorescent calcium indicator (Kd = 115 nM for calcium) that is ideal for monitoring low levels of calcium, as are found in resting cells; may be used to buffer intracellular calcium transients.
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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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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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BQU57
Cayman ChemicalFormal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C16H13F3N4O Formula Weight: 334.3
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Geranylgeranyl Pyrophosphate (ammonium salt)
Cayman ChemicalAn intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.
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AC-55541
Cayman ChemicalA selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC50s = 6.7, 5.9, and 6.6, respectively); elicits pronociceptive activity in vivo.
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AS-1892802
Cayman ChemicalFormal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C20H19N3O2
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CBL0137
Cayman ChemicalA water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM; has broad anticancer activity in mice when administered orally.
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Decitabine
Cayman ChemicalA 2' deoxy analog of 5-azacytidine which is incorporated into DNA and causes hypomethylation by inhibiting DNA methyltransferases in a concentration-dependent manner; useful in conditions characterized by DNA hypermethylation, as is found in myelodysplastic syndromes.
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Stearidonic Acid ethyl ester
Cayman ChemicalAn ester of the free acid that is less water soluble, but more amenable for the formulation of stearidonate-containing diets and dietary supplements.
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PP2
Cayman ChemicalA potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM).
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A-771726
Cayman ChemicalReversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…
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Regadenoson
Cayman ChemicalA selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.
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UNC1999
Cayman ChemicalA selective, cell-permeable EZH2 inhibitor (IC50 = 2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC50 value of 124 nM.
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5-trans Prostaglandin E2
Cayman Chemical5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1. It is 18 times more potent than PGE2 in activating adenylate cyclase in NCB-20 cell homogenates. 5-trans PGE2 accelerates fibrinolysis by enhancing plasminogen activation mediated by…
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16,16-dimethyl Prostaglandin F2ß
Cayman Chemical16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.