Biologically Active Small Molecules, UN2811, Bottle, Glass, Clear
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Doxepin (hydrochloride)
Cayman ChemicalA tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.
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Genipin
Cayman ChemicalA protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…
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4-hydroxy Diclofenac
Cayman ChemicalA CYP2C9 metabolite of the NSAID diclofenac that demonstrates anti-inflammatory and analgesic properties by inhibiting COX and suppressing PGE2 synthesis.
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Paxilline
Cayman ChemicalAn indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).
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(+)-Etomoxir (sodium salt)
Cayman ChemicalAn irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.
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SB 225002
Cayman ChemicalA selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 (IC50 = 22 nM).
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KT195
Cayman ChemicalA selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.
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25-hydroxy Vitamin D3
Cayman ChemicalAn intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.
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DPPH
Cayman ChemicalA cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.
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Cylindrospermopsin
Cayman ChemicalA cyanobacterial toxin that targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), inhibits uridine monophosphate synthase complex activity (Ki = 10 µM), and induces DNA damage.
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17ß-hydroxy Wortmannin
Cayman ChemicalAn analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC50 = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC50 = 1.46 μM).
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Ibotenic Acid
Cayman ChemicalA neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.
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Pargyline (hydrochloride)
Cayman ChemicalPargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…
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Diclofenac-d4
Cayman ChemicalIntended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.
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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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Myriocin
Cayman ChemicalMyriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…
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5-Fluorouracil
Cayman ChemicalA pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.
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Cycloheximide
Cayman ChemicalAn inhibitor of protein synthesis in eukaryotes (IC50 = 5-50 μM) that functions by interfering with translational elongation; can either induce or inhibit apoptosis depending on cell type.
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FCCP
Cayman ChemicalA potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.
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Bupivacaine
Cayman ChemicalAn amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.
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Luotonin A
Cayman ChemicalAn alkaloid that inhibits the growth of mouse leukemia P388 cells (IC50 = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC50 = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…
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XAV939
Cayman ChemicalA small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.
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6-Thioguanine
Cayman ChemicalA thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.
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Ketoprofen
Cayman ChemicalA non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.
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Prostaglandin E1
Cayman ChemicalPGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC50 of PGE1 for the inhibition of ADP-induced human platelet…
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Brevetoxin B
Cayman ChemicalA neurotoxin that binds to voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively; ichthyotoxic at nanomolar concentrations.
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GSK2193874
Cayman ChemicalA potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…
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Quercetin
Cayman ChemicalA flavonoid compound found in the bark and rinds of many plants and fruits.
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Brefeldin A
Cayman ChemicalA natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…
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Carmustine
Cayman ChemicalA nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.
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Capsaicin
Cayman ChemicalThe primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…
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Endothall
Cayman ChemicalAn herbicide that is used to control a wide range of terrestrial and aquatic plants.