Activators & Inhibitors

Activity: CysLT1 antagonist . Function/Pharmacology: Potent (EC50 = 1.3nM) and selective Leukotriene D4 antagonist(LTD4)1 displaying inverse agonist activity2, Blocks binding of LTD4 to human (Ki = 0.22 nM) and guinea pig (Ki = 2.1 nM) lung membranes. Selective for the CysLT1 receptor. Multidrug resistance protein 1 (MRP1) inhibitor.3 Chemical Name: 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid

Activity: FLAP inhibitor . Function/Pharmacology: Inhibitor of leukotriene biosynthesis(IC50 = 2.5 nM in human PMN)1 via 5-lipoxygenase-activating protein (FLAP) inhibition (IC50 = 30 nM)2. Also inhibits PPARα (80% inhibition at 10 µM).3 Chemical Name: 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid

Activity: Topoisomerase I inhibitor . Function/Pharmacology: Camptothecin is a natural product isolated from the chinese Happy tree, Camptotheca acuminate. It is an inhibitor of DNA topoisomerase I. It binds irreversibly to the topoisomerase I /DNA complex preventing DNA re-ligation and generating permanent double strand breaks. Potent antitumor agent. Chemical Name: (S)-4-Ethyl-4-hydroxy-1H-pyrano-[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione

Activity: Kinesin Eg5 inhibitor . Function/Pharmacology: S-Trityl-cysteine is a cell permeable inhibitor of mitotic kinesin Eg5 (IC50 for inhibition of basal ATPase activity = 1 µM; IC50 for inhibition of microtubule-activated ATPase activity = 140 nM). Mean growth concentration (GI50) of 1.31 µM for a panel of 60 different tumor cell lines. Chemical Name: (+)-S-Trityl-L-cysteine

Activity: MMP inhibitor (pan spec.) . Function/Pharmacology: Potent pan-specific inhibitor of matrix metalloproteinases ( MMP3 Ki=0.013 µM). Inhibits MMP-1, -2, -7-10, -12-14 and MMP-20. Attenuates inflammation-induced thermal hyperalgesia. Cell Permeable. Chemical Name: N-Isobutyl-N-(4-methoxyphenylsulfonyl)glycyl hydroxamic acid

Activity: PPARγ agonist . Function/Pharmacology: PPARgamma agonist. Stimulates recruitment of transcriptional coactivators to PPARgamma at 1 µM. Stimulates adipogenesis in human mesenchymal stem cells. Induces apoptosis in a variety of tumor cells lines. Cell permeable. Chemical Name: (±)-5-[4-[(6-Hydroxy-2,5,7,8-tetramethylchroman-2-yl)methoxy]-benzyl]-2,4-thiazolidinedione

Activity: PPARγ agonist . Function/Pharmacology: PPARgamma agonist (EC50=3 µM). Stimulates adipogenesis in human mesenchymal stem cells. Inhibits HUVEC differentiation and angiogenesis. Cell permeable. Chemical Name: (±)-5-[4-(1-Methylcyclohexylmethoxy)-benzyl]thiazolidine-2,4-dione

Activity: G-protein inhibitor . Function/Pharmacology: SCH-202676 is a reversible inhibitor of both agonist and antagonist binding to G protein-coupled receptors (GPCRs).1 IC50’s = 0.1-1.7 µM for nine GPCRs.1 Modification of GPCRs is accomplished via sulfhydryl modification.2,3 Chemical Name: N-(2,3-Diphenyl-1,2,4-thiadiazol-5-(2H)-ylidene)methanamine hydrobromide

Activity: Opioid receptor antagonist . Function/Pharmacology: Opioid antagonist. Very similar activity profile to naloxone however displays slower onset and longer duration of action1. Antagonizes the effects of salvinorin2 (κ-agonist) as well as herkinorin3 (μ-agonist). Has been used as a therapeutic for treatment of alcohol dependence4. Chemical Name: 5(α)-17-(Cyclopropylmethyl)-4,5-epoxy-6-methylene-morphinan-3,14-diol hydrochloride