Biologically Active Small Molecules
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SBFI AM
Cayman ChemicalA membrane-permeant, fluorescent Na+ indicator dye; increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.
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Phomopsin A
Cayman ChemicalA cyclic hexapeptide mycotoxin that binds β-tubulin in a vinca domain; blocks microtubule growth, modulates the dynamics of microtubules, and interferes with mitosis.
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Abiraterone
Cayman ChemicalBlocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC50 = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.
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(R,S)-AMPA
Cayman ChemicalThe defining agonist for the AMPA subgroup of ionotropic glutamate receptors, which mediate excitatory neurotransmission; contains an equal mixture of the active (S)-enantiomer and the inactive (R)-enantiomer.
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Zoniporide (hydrochloride)
Cayman ChemicalSelectively inhibits human NHE-1 with an IC50 value of 14 nM; reduces infarct size in a rabbit myocardial ischemia-reperfusion model without adversely affecting hemodynamics or cardiac function.
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10-Nitrolinoleate
Cayman ChemicalThe product of nitration of linoleate by NO-derived reactive species; activates PPARγ (Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake; can also be metabolized to produce nitrite derivatives which in turn form NO, leading to increased cGMP production.
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Coelenterazine h
Cayman ChemicalA synthetic derivative of native coelenterazine that exhibits 16-fold higher luminescence intensity (emission maximum ~466 nm; half-total time of 0.6-1.2 sec) than native coelenterazine.
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Fenofibrate
Cayman ChemicalA PPARα agonist and hypolipidemic drug used clinically to treat dyslipidemia and cardiovascular disease; exhibits EC50 values of 18 and 30 µM for mouse and human PPARα, respectively.
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Fludarabine
Cayman ChemicalA nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.
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N-phenylacetyl-L-Homoserine lactone
Cayman ChemicalA small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.
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SCR7 pyrazine
Cayman ChemicalA small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC50s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…
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GDC-0941
Cayman ChemicalA potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively; inhibits the growth of certain types of cancer cells, and blocks signaling through PI3K to Akt, both in cells and in vivo.
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ß-Cembrenediol Methyl Ether
LKT Labsβ-cembrenediol is a diterpene product found in tobacco plants and cigarette smoke. β-cembrenediol displays weak anticancer and antimicrobial activity, exhibiting some cytotoxicity in cellular models. Grade: ≥98%
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ß-acetyl-Boswellic Acid
Cayman ChemicalA non-reducing inhibitor of 5-LO that shows selectivity for 5-LO over 12-LO or COX; inhibits topoisomerase II activity and arrests cell cycling or induces apoptosis in cancer cells.
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CAY10505
LKT LabsCAY10505 is an inhibitor of p110? PI3K. CAY10505 increases endothelial relaxation, normalizes levels of glutathione, nitrate, and nitrite, and alters the vascular endothelial lining in hypertensive rats, improving vascular endothelial dysfunction. Grade: ≥98%
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Autocamtide-2-related Inhibitory Peptide
Cayman ChemicalA selective CaMKII inhibitor (IC50 = 40 nM) that was designed based on the sequence around the autophosphorylation site (Thr286/Thr287) in the autoinhibitory domain of the protein kinase.
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Nodularin
Cayman ChemicalA hepatotoxic monocylic pentapeptide that acts as a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively.
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Microcystin-RR
Cayman ChemicalA toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.
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Ampiroxicam
LKT LabsAmpiroxicam is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory and analgesic activities; it inhibits COX-1 and COX-2. Ampiroxicam is a prodrug of piroxicam that does not inhibit prostaglandin synthesis itself. In animal models of inflammation, ampiroxicam decreases…
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17-phenyl trinor Prostaglandin F2a diethyl amide
Cayman ChemicalAn F-series PG analog in which the C-1 carboxyl group has been modified to an N-diethyl amide; dialkyl amides such as a 17-p-PGF2α-NEt2 are inert to corneal amidase activity, and are not converted in any detectable amount to the corresponding free acids.
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2-Acetyl-5-tetrahydroxybutyl Imidazole
Cayman ChemicalAn inhibitor of S1P lyase; treatment of mice (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs, resulting in reversible lymphopenia.
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BMS 303141
Cayman ChemicalA cell-permeable ACL inhibitor (IC50 = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.
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Hygromycin B
Cayman ChemicalAn antibiotic which is used in molecular and cell biology to select for transformed cells expressing the hygromycin resistance gene; kills prokaryotic and eukaryotic cells by inhibiting protein synthesis.
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Piroxicam
Cayman ChemicalAn NSAID that non-selectively and reversibly inhibits both COX isoforms (IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively).
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Cholic Acid 7-sulfate
Cayman ChemicalA naturally occurring metabolite of bile acid that is produced by the conjugation of cholic acid and sulfate, predominantly in the liver and gut.
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Bilirubin
Cayman ChemicalA yellow breakdown product of heme catabolism, formed when heme is cleaved by heme oxygenase; has key roles as a free radical scavenger with antioxidant and anti-inflammatory actions.
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D-myo-Inositol-1,3,4,6-tetraphosphate (ammonium salt)
Cayman ChemicalLargely acts a cell signaling intermediate; serving as substrate to produce IP5s, which can be further phosphorylated to produce Ins(1,2,3,4,5,6-)P6; also phosphorylated to produce phytic acid, which serves diverse roles in eukaryotic tissues; a poor activator of the Ins(1,4,5)-P3 receptor in vitro.
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a-Amanitin
Cayman ChemicalA mycotoxin that selectively inhibits RNA polymerase II (1 µg/ml), preventing translocation of the enzymes on DNA; used in molecular biology to distinguish among types of RNA polymerase in a sample and to arrest RNA synthesis in transcription studies.
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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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22(R)-hydroxy Cholesterol
Cayman ChemicalAn endogenous agonist for LXRα (EC50 = 325 nM) that can induce the expression of the ABCA1 reverse cholesterol transporter to inhibit the overall absorption of cholesterol; used as a substrate to monitor cholesterol transport or as an endogenous positive control for testing LXR agonists.
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SW033291
Cayman ChemicalA potent inhibitor of 15-PGDH (Ki = ~0.1 nM) that has activity in vivo; rapidly increases the levels of PGE2 in bone marrow and other tissues in mice after intraperitoneal injection.