Biologically Active Small Molecules
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8-iso Prostaglandin F1ß
Cayman Chemical8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.
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Calcitonin gene-related peptide (CGRP) is an endogenous neuropeptide that exhibits anti-inflammatory, anti-resorptive, anxiogenic, neuroprotective, and pro-angiogenic activities. In animal models of livery injury, CGRP displays protective benefit, decreasing pro-inflammatory cytokine levels. CGRP…
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15-keto Prostaglandin E2
Cayman ChemicalAn inactive metabolite of PGE2 formed by 15-hydroxy PGDH PGs inactive.
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MIV-150
Cayman ChemicalA tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC50s = 1 nM in vitro).
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Benzydamine Hydrochloride
LKT LabsBenzydamine is a non-steroidal anti-inflammatory drug (NSAID) that also exhibits analgesic, anesthetic, and antibacterial activities. Benzydamine is clinically used to treat mucositis and sore throat. Unlike most NSAIDs, benzydamine inhibits prostaglandin synthetase, not cyclooxygenase (COX).
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Rp-8-CPT-Cyclic AMP (sodium salt)
Cayman ChemicalA lipophilic and non-hydrolyzable cAMP analog that acts as a site-selective inhibitor of PKA type I and II, with preference towards site A of type I and site B of type II.
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N-undecanoyl-L-Homoserine lactone
Cayman ChemicalA homoserine lactone member that possesses a rare odd-numbered acyl carbon chain and may be a minor quorum-sensing signaling molecule in P. aeruginosa strains.
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Cycloguanil (hydrochloride)
Cayman ChemicalAn active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).
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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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Ambroxol Hydrochloride
LKT LabsAmbroxol is a bronchial expectorant that also exhibits antioxidative activity. Ambroxol stimulates the ciliary beat frequency and increases mucous secretion in the lung and trachea. In clinical settings, ambroxol increases levels of thioredoxin and thioredoxin reductase, decreasing oxidative stress…
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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.