Biologically Active Small Molecules, Cayman Chemical, 25 mg
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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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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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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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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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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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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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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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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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Docosapentaenoic Acid methyl ester
Cayman ChemicalA more lipid-soluble form of DPA amenable to analysis using gas chromatography; may serve as a prodrug, since it should facilitate uptake of DPA and then be hydrolyzed by esterases to generate the free acid after uptake into cells.
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Olvanil
Cayman ChemicalA structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum genus, and the amide of vanillylamine and oleic acid; acts as an agonist at TRPV1, inducing desensitization analgesia in rat and mouse models of pain; potentiates the agonist activity of…
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AMC Arachidonoyl Amide
Cayman ChemicalAMC-AA is one of several fatty acid amides which can be used to measure FAAH activity. Exposure of AMC-AA to FAAH results in the release of the fluorescent aminomethyl coumarin that absorbs at 360 nm and emits at 465 nm, allowing for fast and convenient measurement of FAAH activity using a simple…
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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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Methsuximide
Cayman ChemicalA succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.
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CYM 5541
Cayman ChemicalA selective agonist of S1P3 (EC50 = 72-132 nM); less effectively activates S1P1 (EC50 = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.
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Cyclic Pifithrin-a (hydrobromide)
Cayman ChemicalA stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC50 = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…
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DAPI (hydrochloride)
Cayman ChemicalA fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications; characterized by ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths.
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25-hydroxy Cholesterol
Cayman ChemicalA side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of SREBPs; has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor and immunomodulating activities.
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Doripenem
Cayman ChemicalA broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.
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3-Hydroxyglutaric Acid
Cayman ChemicalA metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.
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CAY10449
Cayman ChemicalA potent antagonist for the human IP (prostacyclin) receptor that antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cAMP accumulation in a dose-dependent manner; inhibits the binding of tritiated iloprost to rodent neuroblastoma cells (Ki = ~ 3 nM).
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Abiraterone
Cayman ChemicalBlocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC50 = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.