NEW! Life Science, 5 mg, Biologically Active Small Molecules
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CP 690,550
Cayman ChemicalA potent, cell-permeable inhibitor of all JAK isoforms (IC50 = 6.1, 12, and 8.0 nM for JAK1, JAK2, and JAK3, respectively); useful in ameliorating inflammatory or autoimmune components of a host of diseases.
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Eicosapentaenoyl Ethanolamide
Cayman ChemicalAn N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.
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BQU57
Cayman ChemicalFormal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C16H13F3N4O Formula Weight: 334.3
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Letermovir
Cayman ChemicalA small molecule inhibitor of human cytomegalovirus viral replication (EC50 = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.
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RG-108
Cayman ChemicalA non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.
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Vinclozolin M2
Cayman ChemicalA metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).
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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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GS-5885
Cayman ChemicalAn inhibitor of non-structural protein 5A of hepatitis C virus; effectively reduces or eliminates certain genotypes of hepatitis C virus in vivo, particularly when used in combination with other agents.
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Linolein Hydroperoxides
Cayman ChemicalLinolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…
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NF449 (sodium salt)
Cayman ChemicalAn analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to…
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(±)-ß-Hydroxybutyrate-d4 (sodium salt)
Cayman ChemicalAn internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.
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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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(S)-p38 MAP Kinase Inhibitor III
Cayman ChemicalA methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 µM in vitro); potently blocks the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 µM, respectively).
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Genistin
Cayman ChemicalA natural isoflavone which acts as a phytoestrogen; stimulates the growth of estrogen-dependent breast cancer cells in vivo; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover; increases bone formation in collagen matrix in vivo.
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PFI-3
Cayman ChemicalBinds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.
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CYM 5442
Cayman ChemicalA selective SIP1 agonist (EC50 = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC50 = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.
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SB-525334
Cayman ChemicalA potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.
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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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ß-Zearalenol
Cayman ChemicalA hepatic metabolite of zearalenone that is a less potent agonist of estrogen receptors than the parent compound.
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BQCA
Cayman ChemicalA positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s disease.
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Wogonin
Cayman ChemicalA flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.
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Zearalanone
Cayman ChemicalA major phase I metabolite of the mycotoxin α-zearalanol (zeranol), a non-steroidal estrogen produced by fungi; an estrogen receptor agonist (EC50 = 0.11 µM).
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ONO-8711
Cayman ChemicalA potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO3- secretion in the stomach.
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K252c
Cayman ChemicalK252c is a cell-permeable PKC inhibitor (IC50s = 2.45 and 25.7 µM for PKC and PKA, respectively). It induces apoptosis in human chronic myelogenous leukemia cancer cells. In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains…
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Jacaric Acid
Cayman ChemicalA conjugated PUFA that induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM); increases the production of ROS, leading to oxidative stress that contributes to cytotoxicity.
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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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Oligomycin B
Cayman ChemicalA nonselective inhibitor of the mitochondrial F1FO ATP synthase that can reduce the rate of ATP depletion in myocardial ischemia and decrease calcium-induced calcium release oscillation frequency of rat sensory neurons.
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HE-3235
Cayman ChemicalA synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC50 = 6 nM) and in vivo.
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Febuxostat
Cayman ChemicalA nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.
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Lutein
Cayman ChemicalA natural yellow carotenoid, which can be found in plants, egg yolks, and in the human retina; a lipid-soluble antioxidant that can circulate in the plasma and confer cardioprotective, anti-inflammatory, and anti-angiogenic effects.
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AZD 2932
Cayman ChemicalCAS Number: 883986-34-3 Molecular Formula: C24H25N5O4 Formula Weight: 447.5