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A potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM); also inhibits ERK8, MNK2, Aurora B, Aurora C, MARKs 1-4,TBK1, IKKε, and additional kinases at comparable concentrations.
A structurally unusual antibiotic that inhibits NADH-dependent enoyl (Acyl-Carrier-Protein) reductase InhA, preventing mycolic acid synthesis in M. tuberculosis, including isoniazid-resistant strains (MICs = 0.31-0.63 µg/ml).
Peptide Sequence: human hematopoietic type PGD synthase amino acids 30-41 (EDHRIEQADWPE) To be used in conjunction with Cayman’s hematopoietic type PGD synthase polyclonal antibody (Catalog No. 160013) to block protein-antibody complex formation during analysis for hematopoietic type PGD...
5-trans U-44069 is the C-5 double bond isomer of U-44069. There are no published reports on its biological activities.
A low-calcemic vitamin D receptor agonist; increases keratinocyte differentiation and reduces expression of transcriptional activators in the inflammatory response; induces T-cell differentiation in keratinocytes.
Triamcinolone is a synthetic glucocorticoid.{45390,45393} It increases expression of the calcitonin receptor in murine osteoclast-like cells when used at a concentration of 1 µM.{45391} Triamcinolone (3 mg/kg, s.c.) reduces heat hyperalgesia and mechano-allodynia and decreases the number of...
A potent and selective agonist of the nuclear receptor PPARβ/δ (Ki = 9 nM, EC50 ~500 nM for hPPARβ/δ); less effective against PPARα and PPARγ, with activity at those receptors depending on cell type and system of study.
A natural adenosine analog that prevents IRE1α-induced mRNA cleavage (IC50 = 80 nM) and inhibits constitutive activation of XBP1 in multiple myeloma cell lines; used to study IRE1α action in the endoplasmic reticulum stress response.
A analytical reference material categorized as a phytocannabinoid; considered an impurity in the commercial preparations of cannabidiol; intended for research and forensic applications
Source: Recombinant protein expressed in E. coli Mr: 13.9 kDa Histone 2A is one of the four histones that comprise a nucleosome protein core.
A major metabolite of histamine used as a biomarker of histaminergic system activity.
A highly functionalized and biased thiazole used as a heterocyclic building block to specifically modify lead compounds for drug discovery.
Active recombinant C-terminal His-tagged enzyme expressed in E. coli A bifunctional zinc metalloenzyme that converts LTA4 into LTB4, a potent neutrophil chemoattractant; potential drug target for a variety of indications associated with leukocyte infiltration to sites of inflammation; has...
A potent, semi-synthetic LXR agonist derived from extracts of the mayapple; induces the expression of the ABCA1 reverse cholesterol transporter to increase the efflux of cholesterol from enterocytes and thus inhibits the overall absorption of cholesterol (ED50 = 1 nM).
A selective, active-site directed, irreversible inhibitor of cPLA2 and iPLA2; inhibits A23187-induced arachidonic acid release from human platelets (IC50 = 0.6 µM) and iPLA2 release from P388D1 cells (IC50 = 0.5 µM); a potent inhibitor of FAAH (IC50 = 2.5...
A fluorescently-tagged probe which allows the HSL molecule to be detected using fluorescence-based techniques.
An inhibitor of Nrf2-induced gene transcription at the antioxidant response element in cells at 1 to 10 µM; sensitizes lung carcinoma A549 cells to chemotherapeutic agents and inhibits the growth of A549 cells in vitro and in vivo in animals.
An analog of AEA in which the alcohol of the ethanolamide group has been replaced with a fluorine atom, which increases the binding affinity and selectivity for the CB1 receptor; in vivo activity is enhanced much less than the binding affinity, because it is rapidly hydrolyzed by FAAH.
A S-nitrosothiol that acts as an NO donor under acidic conditions; decomposes with a half-life of 130 minutes in 0.1 M phosphate buffer, pH 5.0, at 37°C; relaxes phenylephrine-constricted rat aortic strips 71% and 44% at pH 6.0 and 7.4, respectively.
The trans isomer of PGD2 occurs as an impurity between 2-5% in most commercial preparations of the bulk drug product. This compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of...
A acemic monohydroxy fatty acids resulting from the non-enzymatic oxidation of linoleic acid.
A selective, irreversible inhibitor of FAAH (IC50 = 7.2 nM); 0.1 mg/kg reduces inflammatory pain in a rat model.
A potent and selective antagonist of the EP4 receptor (Ki = 13 and 20 nM for human and rat EP4, respectively); inhibits PGE2-evoked elevation in intracellular cAMP in cells and, in vivo, reduces thermal hyperalgesia induced by intraplantar injection of PGE2.
A biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.