93435 Results for: "2-(4-Hydroxyphenyl)ethanol&pageNo=9"

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An excellent affinity ligand for chromatographic purification of protein kinases. Inhibits protein kinases (Ki's: PKA=1.9 µM; PKC=18 µM; PKG=0.87 µM; MLCK=70 µM).

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Selective, potent cAMP-specific phosphodiesterase inhibitor (PDE IV, IC50=2µM). Inhibits superoxide generation and platelet aggregation stimulated by arachidonic acid. Also inhibits fMLP-induced neutrophil adhesion to vascular endothelial cells.

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PKC inhibitor

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EGFR inhibitor

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Inhibitor of PP1 and PP2A

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Inhibits angiogenesis

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Adenylate cyclase inhibitor

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Methionine aminopeptidase 2 inhibitor

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Adenylate cyclase activator

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Anandamide transport inhibitor

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A cell-permeable cGMP antagonist which is resistant to hydrolysis by cyclic nucleotide phosphodiesterases (Ki=0.5 µM). No metabolic side effects. Significantly more lipophilic and membrane permeant as compared to Rp-cGMPS or Rp-8-Br-cGMPS

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Cannabinoid receptor ligand.

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Acyl-CoA synthetase inhibitor

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PKC inhibitor

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Inhibitor of non-muscle myosin II

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Ikarugamycin inhibits the uptake of oxidized low-density lipoprotein in mouse macrophages. It blocks PMA and Nef-mediated cell surface CD4 down-regulation. Ikarugamycin is emerging as a general inhibitor of clathrin-coated pit-mediated endocytosis and appears to be a useful agent for studying the process of endocytosis.

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Potent, cell permeable, selective, and reversible inhibitor of c-Jun N-terminal kinase (JNK) (IC50=40nM for JNK-1 and JNK-2 and 90nM for JNK-3). The inhibition is competitive with respect to ATP. Exhibits over 300-fold greater selectivity for JNK as compared to ERK1 and p38. Inhibits the phosphorylation of c-Jun and blocks the expression of IL-2, IFN-γ, TNF-α, and COX-2. Blocks IL-1-induced accumulation of phospho-Jun, induction of c-Jun transcription and anti CD3-induced apoptosis of CD4+ CD8+ thymocytes.

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Highly potent inhibitor of VEGFR-1 (IC50=130nM), VEGFR-2 (IC50=23nM) and VEGFR-3 (IC50=18nM). At higher concentrations it inhibits PDGFR-β (640nM), c-Kit (236nM) and CSF-1R (380nM).

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Cytochrome P450 inhibitor

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Competitive, mechanism-based inhibitor of matrix metalloproteinases 2 and 9 (MMP-2 and MMP-9). It possesses Ki values in the nanomolar range against the gelatinases (14nM for MMP-2; 600nM for MMP-9), but in the micromolar range against other metalloproteinases (206µM for MMP-1, 15µM for MMP-3, 96µM for MMP-7, and 4µM for ADAM17/TACE). This inhibitor has also been used in vitro, in vivo, and in tissue culture. In vivo, it is metabolized to an even more potent gelatinase inhibitor.

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BIBB 515 is a potent and selective inhibitor of 2,3-oxidosqualene cyclase (OSC) in vivo. BIBB 515 inhibits LDL production in both normolipemic and hyperlipemic hamsters and may represent a novel approach for the development of lipid lowering drugs.

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High potency synthetic agonist at GPR40.

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Retinoic acid receptor ligand.

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Eicosapentaenoyl ethanolamide ≥98% (by TLC)

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Potent inhibitor of farnesyltransferase in isolated enzyme assays (IC50=30 nM) and in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II (IC50=35.8 µM and 67 µM respectively). α-Hydroxyfarnesylphosphonic acid inhibited (1 µM) Ras processing in Ha-ras-transformed NIH 3T3 fibroblasts.

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CaM kinase kinase inhibitor

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Unsaturated analog of endogenous sleep inducing lipid.

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Potent, dual site (ATP domain and substrate-binding domain) Src and Lck kinase inhibitor (IC50=44 and 88nM respectively). VEGFR2 IC50=0.32μM; c-fms IC50=30μM.

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Potent, selective and irreversible inhibitor of MAG lipase (IC50=8nM vs 4µM for FAAH). JZL-184-treated mice displayed a number of CB1-dependent behavioral effects including analgesia, hypothermia and hypomotility as well as increased levels of 2-arachidonoylglycerol in the brain ( approx. 8-fold, with no effect on anandamide levels). JZL-184 produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice. It blocks neuropathic pain and enhances retrograde endocannabinoid signaling.

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BML-277 is a highly selective inhibitor of Chk2 (IC50=15nM). It displays potent radioprotective activity and prevents apoptosis of human T cells subjected to ionizing radiation (EC50= 3-7.6µM). Useful tool for dissecting the role of Chk2 in cellular signaling.