Biologically Active Small Molecules
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5-iPF2a-VI
Cayman ChemicalIsoprostanes are prostaglandin (PG)-like products of free-radical induced lipid peroxidation. Although the isoprostanes derived from arachidonic acid are the best characterized, many other polyunsaturated fatty acids can form isoprostanes. iPF2α-VI is one of dozens of possible stereo- and…
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2-O-ethyl PAF C-16
Cayman Chemical2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…
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L-(+)-Ergothioneine
Cayman ChemicalA naturally-occurring amino acid which is a stable antioxidant; scavenges free radicals and oxidants, controls NF-κB activation, and inhibits inflammatory gene expression; blocks oxidative DNA damage and cell death.
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AT7519 (hydrochloride)
Cayman ChemicalAn ATP-competitive inhibitor of Cdk1, 2, 4, 5, 6, and 9 with IC50 values of 210, 47, 100, 13, 170, and 50s = 40-940 nM in vitro) and human tumor xenograft models, inhibiting cell cycle progression and inducing apoptosis.
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Amitriptyline Hydrochloride
LKT LabsAmitriptyline exhibits antidepressant, antipsychotic, analgesic, and antinociceptive activities; it acts as an antagonist at 5-HT2A/2C/6/7 receptors, M1-5 muscarinic acetylcholine receptors (mAChRs), H1/4 histamine receptors, a1-adrenergic receptors, and also on the serotonin transporter (SERT) and…
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Coumarin Boronic Acid pinacolate ester
Cayman ChemicalA fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.
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Erbstatin Analog
Cayman ChemicalA stable, potent analog of erbstatin; inhibits EGFR tyrosine kinase in vitro with an IC50 of 0.14 µg/ml; inhibits EGF-stimulated growth in NIH3T3 cells with an IC50 value of 0.5 µg/ml; delays onset of EGF-induced DNA synthesis.
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5-fluoro 203
Cayman ChemicalA cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…
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Glufosinate (ammonium salt)
Cayman ChemicalA racemic mixture of D- and L-phosphinothricin, used as the active ingredient in broad spectrum herbicides; also used, with the bar gene, which encodes phosphinothricin acetyltransferase, for selection during genetic engineering in plants.
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ZLN005 (hydrochloride)
Cayman ChemicalA small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…
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BPIQ-I
Cayman ChemicalA quinazoline that inhibits the tyrosine kinase activity of EGFR (IC50 = 0.025 nM); inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC50s = 6.5 and 30 µM, respectively).
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Zileuton
Cayman ChemicalZileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…
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(±)14(15)-EpEDE
Cayman ChemicalAn EpEDE acid formed from DGLA, either by a strong oxidizing agent or by cytochrome P450 epoxygenases; biological properties are poorly understood.
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ISCK03
Cayman ChemicalA cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.
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SB-743921 (hydrochloride)
Cayman ChemicalCAS Number: 940929-33-9 Molecular Formula: C31H33ClN2O3 • HCl Formula Weight: 553.5
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C-6 NBD Ceramide
Cayman ChemicalC-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…
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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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Everolimus
Cayman ChemicalA hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM; orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.
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Vitexin
Cayman ChemicalAn apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.
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15(R)-Lipoxin A4
Cayman ChemicalAn aspirin-triggered lipoxin that inhibits LTB4-induced chemotaxis, adherence, and transmigration of the neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.
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Dihydroartemisinin
LKT LabsDihydroartemisinin is a sesquiterpene lactone that can be derived from Artemisia. Dihydroartemisinin exhibits anticancer, antiviral, anti-inflammatory, anti-asthma, and anti-parasitic activities. Artemisinins such as dihydroartemisinin are best known for their antimalarial activity.…
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Nisin A
Cayman ChemicalA bacteriocin, a natural polycyclic antibacterial peptide, also called a lantibiotic; particularly effective against Gram-positive bacteria and commonly used as a food preservative.
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ß-Estradiol
MP Biomedicalsβ-estradiol is a potent mammalian estrogenic hormone produced by the ovary. Triggers the production of gonadotropins leading to ovulation. β-Estradiol is used to study cell differentiation and transformations (tumorigenicity). The pharmacology and HPLC determination of β-Estradiol…
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3-bromo-5-phenyl Salicylic Acid
Cayman ChemicalSelective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC50 = 460 nM).
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AS-1892802
Cayman ChemicalFormal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C20H19N3O2
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Obatoclax (mesylate)
Cayman ChemicalAn antagonist of Bcl-2 family members containing four Bcl-2 homology domains, including Bcl-2, Bcl-W, Bcl-xL, and Mcl-1 (Kd ~500 nM); prevents interaction of these pro-survival proteins with Bax or Bak, inducing apoptosis; also induces autophagy in mouse embryo fibroblasts and in HeLa cell.
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AGDV
LKT LabsAGDV is a C-terminal peptide sequence found on fibrinogen that is known as a binding site for glycoprotein IIb/IIIa (integrin aIIbß3); this binding is required for platelet adhesion and aggregation.
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Cysmethynil
Cayman ChemicalAn indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells.
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Cefapirin
Cayman ChemicalA first generation cephalosporin antibiotic that is broadly effective against gram-negative and gram-positive bacteria; mainly used in veterinary medicine for intramammary treatment of mastitis and intrauterine treatment of endometritis in cattle.
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EPZ015666
Cayman ChemicalA potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.
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