Biologically Active Small Molecules
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ThioFluor 623
Cayman ChemicalReacts with thiols resulting in an increase in fluorescence intensity of up to 120-fold; the response is selective for thiols, occurs in aqueous media, and results in a fluorophore with emission at 623 nm; cell-permeable.
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CAY10444
Cayman ChemicalA selective antagonist of S1P binding to the S1P3 receptor; blocks calcium increase in HeLa cells by about 40% at 10 µM.
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PTC-124
Cayman ChemicalA nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC50 = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…
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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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Estradiol 17-(ß-D-Glucuronide) (sodium salt)
Cayman ChemicalAn estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.
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4-hydroxy Nonenal Mercapturic Acid-d3
Cayman ChemicalAn internal standard for the quantification of 4-HNE mercapturic acid by GC- or LC-MS.
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4-Methylumbelliferyl 6-thio-Palmitate-ß-D-Glucopyranoside
Cayman ChemicalA fluorogenic substrate of palmitoyl-protein thioesterase.
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Gly-Phe-ß-naphthylamide
Cayman ChemicalA substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.
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11ß-13,14-dihydro-15-keto Prostaglandin F2a
Cayman ChemicalA metabolite of PGD2 via the 15-hydroxy PGDH pathway.
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L-Leucine 4-methoxy-ß-naphthylamide (hydrochloride)
Cayman ChemicalA cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.
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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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CBFß Inhibitor
Cayman ChemicalA small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 µM); blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.
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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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PDM 11
Cayman ChemicalA structural analog of several resveratrol derivatives which act as a potent and selective AhR antagonists and agonist.
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Doxorubicin (hydrochloride)
Cayman ChemicalAn anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.
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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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Isovaleroylglycine
Cayman ChemicalUrinary metabolite of leucine that is used as a diagnostic tool in the diagnosis of various acidemias and mitochondrial fatty acid β-oxidation defects.
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PF-04620110
Cayman ChemicalA potent and selective inhibitor of DGAT-1 (IC50 = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.
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Oleic Acid-2,6-diisopropylanilide
Cayman ChemicalACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…
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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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TBB
Cayman ChemicalAn ATP/GTP-competitive inhibitor of CK2 (IC50 = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC50 = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.
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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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Sinensetin
Cayman ChemicalA polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.
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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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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.