Biologically Active Small Molecules, 1 mg
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4ß-hydroxy Cholesterol
Cayman ChemicalA major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.
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T0070907
Cayman ChemicalA potent and selective PPARγ antagonist with an apparent IC50 value of 1 nM for the human receptor.
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SB 290157 (trifluoroacetate salt)
Cayman ChemicalA non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM; potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM); also effective in vivo, reducing inflammation…
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4-Methylumbelliferyl 6-thio-Palmitate-ß-D-Glucopyranoside
Cayman ChemicalA fluorogenic substrate of palmitoyl-protein thioesterase.
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Prostaglandin F2ß (tromethamine salt)
Cayman ChemicalA derivative of PGF2β with increased water solubility.
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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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11-deoxy Prostaglandin F1ß
Cayman Chemical11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 µg/kg.
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ML-191
Cayman ChemicalAn antagonist of GPR55, blocking LPI-induced activation (EC50 = 1.1 µM); has minimal effect at the GPR35 and CB2, although it acts as a weak antagonist of CB1 (IC50 = 17.7 µM); inhibits LPI-induced phosphorylation of ERK1/2 and blocks receptor-dependent…
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5-trans Prostaglandin E2
Cayman Chemical5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1. It is 18 times more potent than PGE2 in activating adenylate cyclase in NCB-20 cell homogenates. 5-trans PGE2 accelerates fibrinolysis by enhancing plasminogen activation mediated by…
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DAN-1 EE (hydrochloride)
Cayman ChemicalDAN-1 EE is a fluorescent indicator for the bioimaging of NO. DAN-1 EE is a cell permeable derivative of DAN, a molecule which has been used extensively in the quantitation of nitrate and nitrite using fluorescence spectroscopy. Upon entry into the cell, DAN-1 EE is transformed into the less cell…
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(Z)-4-hydroxy Tamoxifen
Cayman ChemicalA major phase I metabolite of tamoxifen, a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium; has at least a 100-fold higher affinity for estrogen receptors than tamoxifen.
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Simvastatin (sodium salt)
Cayman ChemicalA potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.12 nM).
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(R)-(+)-Eicosapentaenyl-1'-Hydroxy-2'-Propylamide
Cayman ChemicalA homolog of EPEA, characterized by the addition of an (R)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.
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PFI-4
Cayman ChemicalA chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21); potent in cells, with an IC50 value of 250 nM.
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Ac-YVAD-pNA
Cayman ChemicalA colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.
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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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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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4-Nitrophenyl ß-D-Cellotrioside
Cayman ChemicalA chromogenic substrate for endoglucanases and cellobiohydrolases.
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Chaetoglobosin A
Cayman ChemicalA mycotoxic cytochalasin that targets filamentous actin and demonstrates antibacterial and nematicidal effects as well as induces apoptosis in cancer cell lines.
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Atglistatin
Cayman ChemicalA potent, selective, and competitive inhibitor of ATGL (IC50 = 0.7 μM); does not inhibit hormone-sensitive lipase, monoglyceride lipase, pancreatic lipase, lipoprotein lipase, or other lysophospholipases; blocks lipolysis by ATGL in vitro, in white adipose tissue organ cultures, and…
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Clasto-Lactacystin ß-lactone
Cayman ChemicalActive metabolite of lactacystin, a widely used selective inhibitor of the 20S proteasome, with at least 10 times better activity; irreversibly alkylates subunit X of the 20S proteasome.
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Octyl-a-ketoglutarate
Cayman ChemicalA stable, cell-permeable form of α-ketoglutarate which accumulates rapidly and preferentially in cells with a dysfunctional TCA cycle; stimulates PHD activity and increases HIF-1α turnover when used at 1 mM; competitively blocks succinate- or fumarate-mediated inhibition of PHD.
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PHA-767491
Cayman ChemicalAn inhibitor of Cdc7 kinase (IC50 = 10 nM) as well as Cdk9, (IC50 = 34 nM); induces apoptotic cell death in multiple cancer cell types at 10 µM.
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Ac-DEVD-pNA
Cayman ChemicalA para-nitro aniline chromophore cleaved by caspases (Km = 18, 11, 32, 180, and 12 µM for caspases-1, -3, -4, -6, and -7, respectively); not cleaved by caspase-2; monitored colorimetrically at 405 nm.
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Prostaglandin A2-d4
Cayman ChemicalAn internal standard for the quantification of PGA2 by GC- or LC-MS.
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11-keto-ß-Boswellic Acid
Cayman Chemical11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). Boswellic acids are specific, non-redox inhibitors of leukotriene synthesis via 5-lipoxygenase that demonstrate anti-inflammatory…
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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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Wnt-C59
Cayman ChemicalA potent inhibitor of PORCN (IC50 = 74 pM), completely blocking Wnt secretion into culture media; prevents activation of all evaluated Wnt family members; effective in vivo as well as in vitro; blocks the progression of breast cancer while downregulating Wnt/β-catenin pathway target…