Biologically Active Small Molecules
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Ras Inhibitory Peptide
Cayman ChemicalA synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2; specifically blocks the interaction of Sos1 with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases.
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CAY10508
Cayman ChemicalA potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.
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Concanavalin A from Canavalia ensiformis seeds (jack beans)
MP BiomedicalsPure Canavalia ensiformis lectin (Con A) from Jackbean. Isolated by affinity chromatography on cross-linked dextran. Con A exists as a dimer below pH 5.0 and and at pH >7 it exists as a tetramer. Con-A is not a glycoprotein. The monomeric molecular weight of Con-A is 25,500. Con-A does not…
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Paclitaxel
Cayman ChemicalA potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…
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Xanthorrhizol
Cayman ChemicalAn antibiotic that suppresses the expression of ODC, COX-2, and iNOS at concentrations as low as 0.3 μM and exhibits an anti-metastasis effect and anti-tumor promoter activity in various carcinogenesis mouse models.
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Methotrexate
Cayman ChemicalAn analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…
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Carvedilol Phosphate Hemihydrate
LKT LabsCarvedilol phosphate is a cardioprotective a1- and ß1/2-adrenergic receptor inhibitor used to treat congestive heart failure; its inhibitory action at adrenergic receptors slows heart rhythm, decreasing force, pressure, and cardiac workload. Carvedilol phosphate also inhibits release of…
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ALK5 Inhibitor II
Cayman ChemicalA selective inhibitor of the TGF-β type1 receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…
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Aflatoxin B2
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin B2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.
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Nitrendipine
Cayman ChemicalA dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A1, A2A, and A3 receptors with Ki values of 8.96, 23.0, and 8.3 µM, respectively.
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Apamin
Cayman ChemicalA potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3 (IC50 values are 0.06-0.4, 1-12, and 1-13 nM, respectively); ineffective against SK4 at 1 µM.
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LY255283
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 =…
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4-deoxy Nivalenol
Cayman ChemicalA natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.
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Formoterol (hemifumarate)
Cayman ChemicalAn agonist of β-adrenergic receptors that activates the β1, β2, and β3 receptors with pEC50 values of 7.5, 9.0, and 6.8 respectively; displays high selectivity for β-adrenoceptors in the trachea over those in atria; activity is retained in the airway for extended periods.
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Ku-55933
Cayman ChemicalA potent ATP-competitive inhibitor of ATM kinase (IC50 = 13 nM; Ki = 2.2 nM); sensitizes cells to both ionizing radiation and chemotherapeutic agents; induces senescent breast, lung, and colon carcinoma cells to undergo cell death; inhibits HIV-1 replication in C8166 human T-lymophocyte…
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DL-Glyceraldehyde-3-phosphate
Cayman ChemicalAn intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.
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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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Phosphoramidon (sodium salt)
Cayman ChemicalA natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.
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D-erythro-MAPP
Cayman ChemicalAn analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.
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Ac-YVAD-CMK
Cayman ChemicalA selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.
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(±)18-HETE
Cayman ChemicalThe racemic version of a CYP450 metabolite of arachidonic acid that dose-dependently stimulates vasodilation of the rabbit kidney.
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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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Daidzein
Cayman ChemicalAn isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.
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4EGI-1
Cayman ChemicalAn inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.
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CAY10704
Cayman ChemicalA potent inhibitor of HCV infection (EC50 = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC50 = 21.3 µM); displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without…
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Fluvoxamine (maleate)
Cayman ChemicalA selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.
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Omeprazole
Cayman ChemicalA selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).
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Sumatriptan (succinate)
Cayman ChemicalA serotonin 5-HT1B and 5-HT1D receptor agonist (IC50s = 9.3 and 7.3 nM, respectively) that also has affinity for the 5-HT1F receptor (IC50 = 17.8 nM); constricts human middle meningeal arteries (EC50 = 89.9 nM) and reduces vascular inflammation associated with migraines.
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Stigmasterol
Cayman ChemicalA natural plant sterol that can be isolated from certain seed oils and herbs, including those used for therapeutic purposes.
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L-Acetylcarnitine (hydrochloride)
Cayman ChemicalAn acetylated form of L-carnitine that facilitates the uptake of acetyl CoA into mitochondria during fatty acid oxidation, enhances acetylcholine production, and stimulates protein and membrane phospholipid synthesis.
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Adrenorphin
LKT LabsAdrenorphin is an endogenous opioid peptide produced from cleavage of proenkephalin A. Adrenorphin acts as an agonist at ?-opioid receptors (?ORs) and µ-opioid receptors (µORs). Like other opioids, adrenorphin exhibits analgesic, antinociceptive, and gastrointestinal motility modulating…
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trans-Resveratrol-d4
Cayman ChemicalAn internal standard for the quantification of trans-resveratrol by GC- or LC-MS.