94231 Results for: "2-Iodo-3-nitrobenzyl+bromide&pageNo=9"

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Benzodiazepine receptor ligand.

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Antibiotic possessing weak in vitro antimicrobial activity against gram positive bacteria and fungi. A highly selective divalent cation ionophore, commonly used to increase intracellular Ca^2⁺ levels in intact cells.

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Major metabolite of vitamin D3. Mediates calcium and phosphorous homeostasis. Inhibits 1α,25-dihydroxyvitamin D3 and testosterone potentiation of calcium channels in osteosarcoma cells.

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Biosynthesis via liver and renal cytochrome P-450. Induces glucagon release from pancreatic islets. Vasodilator in intestinal microcirculation. Inhibits Na+K+-ATPase. Urinary excretion in humans is increased during pregnancy-induced hypertension.

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Precursor to 1α,25-dihydroxyvitamin D₃

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Lipoxygenase inhibitor

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NMDA receptor antagonist.

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A potent and specific substrate analog PLA2 inhibitor (IC50=6.2 µM-porcine pancreatic PLA2). It inhibits human recombinant sPLA2 (IC50=13.7 µM) selectively over cPLA2. At 1 µM it completely blocked the myogenic response in perfused dog renal arcuate arteries.

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Cytochrome P450 inhibitor

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Sulfur containing antibiotic. Potent inhibitor of bacterial and yeast RNA polymerases. Inhibits mRNA chain elongation. Inhibits adhesion of endothelial cells (HUVECs) to vitronectin (IC50=0.83 µM) thereby inhibiting tumor cell-induced angiogenesis in vivo. Inhibits transcription in C. albicans. Inhibits microbiological growth in beer. Active against soil borne pathogens.

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CCR8 activator.

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A cell-permeable cGMP analog which is more resistant to phosphodiesterases than cGMP and which preferentially activates cGMP-dependent protein kinase. It inhibits thrombin stimulated arachidonic acid release in human platelets.

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MPTP inhibitor

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CDK inhibitor

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ATPase inhibitor

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Macrolide antibiotic that acts as a potent and selective inhibitor of vacuolar-type H⁺-ATPase (V-type) (IC₅₀=004 - 0.4 nmol/mg). Valuable tool for distinguishing among different types of ATPases. Inhibitor of endosomal acidification. Blocks lysosomal cholesterol trafficking in macrophages. Blocks pH regulation in brain cells.

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Clinically useful diuretic. Clopamide selectively inhibits the chloride the sodium chloride cotransporter.

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A rare plant amino acid that reversibly blocks the cell cycle at G1-phase. Inhibits the hydroxylation of deoxyhypusine and thus inhibits eukaryote initiation factor 5-A (eIF5-A). Inhibitor of mammalian tyrosinase and dopamine β-hydroxylase. Also chelates iron via the kojic acid metal-binding domain. Arrests DNA synthesis by inhibiting deoxyribonucleotide metabolism.

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Phospholipase inhibitor

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Member of the tyrphostin family of tyrosine kinase inhibitors. Selective inhibitor of the PDGF receptor kinase (IC50=20µM) vs. the EGF receptor kinase (IC50=820µM). Inhibits PDGF-induced mitogenesis in human bone marrow fibroblasts.

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Cyclooxygenase inhibitor. Selectively inhibits PGH synthase-2 (IC50=1 µM) with no inhibition of PGH synthase-1 at concentrations up to 100 µM. Protects neuronal cultures from LPS-induced neurotoxicity.

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Inhibits PKCα (IC50=43 µM) and PKCγ (IC50=50 µM) without inhibiting the δ, βI and βII isotypes.

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AG-490 is a potent inhibitor of the JAK-2 tyrosine kinase. In acute lymphoblastic leukemia (ALL) cells, which abundantly express JAK-2, AG-490 dose-dependently inhibited DNA synthesis, blocked cell growth and induced apoptosis. At 5 µM, AG-490 almost completely blocked the growth of all pre-B ALL cells but had no significant effect on the growth of mitogen-stimulated normal B or T cells, B-cell lymphoma or T-cell leukemia cells. AG-490 does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src. It blocks interleukin-7-induced JAK kinase activity in T-cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. AG-490 is cell permeable and is a valuable tool for studying the cellular role of JAK kinases in signal transduction.

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Src kinase inhibitor

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Inhibits Rho kinase (ROCK; Ki=0.33μM). Selective protein kinase A and G inhibitor (both Ki’s = 1.6μM). Inhibits agonist-induced activation of NADPH oxidase in human neutrophils (IC50=15μM). Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca2+ antagonist with antivasospastic properties.

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Inhibits ERK2 (Ki = 525nM). Also inhibits adenosine kinase (Ki = 30nM), CK1 and CK2 and insulin receptor kinase (IC50 ranging from 0.4-28µM).

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Potent and specific inhibitor of the protein kinase c-Raf (IC50=70nM). Has no significant effect on many other protein kinases tested (even at 50µM) with the exception of p38 (SAPK2a) (IC50=2µM) and SAPK2b (p38β) (IC50=2µM). Induces a paradoxical >100-fold activation of c-Raf in whole cells.

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ADP-ribosylation factor inhibitor

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GEF inhibitor

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Blocks agonist and antagonist binding to G protein-coupled receptors.