Cayman Chemical Biologically Active Small Molecules
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Suc-AAPF-pNA
Cayman ChemicalA chromogenic substrate that can be cleaved by cathepsin G (Km = 1.7 mM), subtilisins, chymotrypsin (Km = 60 µM), chymase (Km = 4 mM), and cyclophilin; used for inhibitor screening and kinetic analysis.
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Prostaglandin F1ß
Cayman ChemicalPGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.
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Furegrelate (sodium salt)
Cayman ChemicalFuregrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC50 value is 15 nM for human platelet microsomal thromboxane synthase.
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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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Chymostatin
Cayman ChemicalA potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.
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Tamoxifen
Cayman ChemicalA selective estrogen receptor (ER) modulator; an ER antagonist in breast tissue, effective in treating early breast cancer; an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues.
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20-hydroxy N-Arachidonoyl Taurine
Cayman ChemicalA potential cytochrome P450 metabolite of N-arachidonoyl taurine that may activate TRPV1 and TRPV4.
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Ciclesonide
Cayman ChemicalA corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.
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Docetaxel
Cayman ChemicalA semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.
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N-(3-hydroxyphenyl)-Arachidonoyl amide
Cayman Chemical3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.
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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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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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Brilliant Blue G
Cayman ChemicalA dye which stains proteins in gels with ease and sensitivity; used in the Bradford to quantify the amount of protein in a solution; selectively inhibits P2X7 (IC50s = 10.1 nM and 265 nM for rat and human P2X7, respectively) and reduces neurological injury secondary to traumatic brain…
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SL 0101-1
Cayman ChemicalA kaempferol glycoside that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC; inhibits the proliferation of MCF-7 breast cancer cells at 100 μM and attenuates angiotensin II-induced cell…
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(±)11(12)-EpETE
Cayman ChemicalAn epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo; its effects of remain to be determined.
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Sodium Phosphate Stock Solution (500 mM, pH 9.0)
Cayman ChemicalSodium Phosphate Stock Solution (500 mM, pH 9.0) contains filtered 500 mM sodium phosphate buffer. It is ready to use as supplied.
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Arachidonoyl p-Nitroaniline
Cayman ChemicalApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…
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HA-155
Cayman ChemicalA selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.
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Biocytin
Cayman ChemicalA conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.
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Puromycin (hydrochloride)
Cayman ChemicalAn aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.
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DY 131
Cayman ChemicalA selective ERRβ/γ receptor agonist (EC50 = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.
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2-hydroxy Flutamide
Cayman ChemicalThe major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900), blocking the expression of AR target genes.
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CX-5461
Cayman ChemicalA selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC50s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.
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(±)10(11)-EpDPA
Cayman ChemicalA DHA epoxygenase metabolite detected in rat brain and spinal cord, as well as human serum, that acts as a substrate for sEH (Km = 5.1 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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Tivantinib
Cayman ChemicalA staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM).
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Docosahexaenoyl Ethanolamide
Cayman ChemicalThe ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…
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DL-AP5
Cayman ChemicalThe racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.
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SMI-4a
Cayman ChemicalA Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK, killing a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM); induces G1 phase cell-cycle arrest, dose-dependent induction of p27Kip1, apoptosis through the mitochondrial…
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BW 245C
Cayman ChemicalBW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…
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Cytochalasin B
Cayman ChemicalA cell-permeable mycotoxin which binds to the barbed end of actin, reversibly inhibiting the elongation and shortening of actin filaments; blocks diverse cellular functions, including cell division, migration, phagocytosis, exocytosis, chemotaxis, and glucose transport.