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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2-phenyl-3-methyl-Quinoxaline
Cayman ChemicalA synthetic intermediate useful for pharmaceutical synthesis.
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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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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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Tetrodotoxin
Cayman ChemicalA potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.
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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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Berberine Chloride
LKT LabsBerberine is an isoquinoline alkaloid found in a variety of plants, including barberry, goldenseal, Oregon grape, California poppy, and the Amur cork tree. Berberine fluoresces under ultraviolet light and is often used to stain heparin in mast cells. Berberine displays many beneficial effects,…
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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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Ursolic Acid
Cayman ChemicalA natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…
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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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Tetrodotoxin Citrate
Cayman ChemicalA potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.
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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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Amphotericin B
Cayman ChemicalA polyene macrolide used in the treatment of infections caused by C. albicans, A. fumigatus, and parasitic L. protozoans, as well as in tissue culture to prevent fungi from contaminating cell cultures; binds with ergosterol in fungal cell membranes, altering membrane permeability and ultimately…
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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.