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Cocktails, tablets, capsules, and individual purified formulations of protease inhibitors and phosphatase inhibitors designed to protect proteins from degradation during cell lysis and extraction.
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An ENPP1 inhibitor (IC50 = 0.188 µM); inhibits ENPP1 in MDA-MB-231 cells (IC50 = 0.732 µM); selectively cytotoxic to 4T1 murine metastatic breast cancer cells (IC50 = 2.99 µM) over non-cancerous L-02 and 293T cells at 50 µM; increases serum levels of IFN-β in mice when administered at a dose of 0.5 mg/kg in combination with cGAMP
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Leupeptin hemisulfate (Ac-Leu-Leu-argininal) is a reversible inhibitor of serine and cysteine endopeptidases Leupeptin hemisulfate is capable of inhibiting plasmin trypsin papain kallikrein calpain and cathepsin B Leupeptin is usually used in a concentration range of 10 to 100 M Leupeptin is widely used in many protease inhibitor cocktails due to its potency low toxicity and range of inhibition Leupeptin is also used in a quantitative assay to measure macroautophagic flux in mammals and is being investigated for its use in treating malaria
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Sensitive substrate for continuous assays and in situ determination of the matrix metalloproteinase activity. When cleaved at the Gly-Leu bond it separates the highly fluorescent Mca group from the efficient 2,4-dinitrophenyl quencher and results in the increase of fluorescence intensity. The kcat/km value for the punctuated metalloproteinase (MMP-7) and for gelatinase (MMP-2), e.g., are 1.7 x 105 and 6.3 x 105 M-1s-1, respectively. ONE-LETTER SEQUENCE: Mca-PLA-Nva-Dap(Dnp)-AR-NH2MOLECULAR FORMULA: C49H68N14O15MOLECULAR WEIGHT:1093.16STORAGE CONDITIONS: -20 5C, CAS REGISTRY NUMBER: [256394-92-0], SYNONYMS: Mca-Pro-Leu-Ala-Nva-Dap(Dnp)-Ala-Arg-NHRESEARCH AREA: CancerREFERENCES: G. Murphy, et al., J. Biol. Chem. 269, 6632 (1994)
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Protease inhibitor. Inhibitor of serine proteinases having a chymotrypsin-like specificity like α-, β-, δ- and γ-chymotrypsin, chymases, cathepsin G, and most cysteine proteinases including papain and cathepsin A, B, H, and L. Mixture of type A (R=L-Leu), type B (R=L-Val), type C (R=L-Ile). Alternative name: (S)-1-Carboxy-2-phenylethyl)-carbamoyl-alpha-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal. Formula: C21H38N4O8. MW: 605.0 (average). Solubility: Soluble in DMSO (20mg/ml) or glacial acetic acid. Long Term Storage: -20°C.
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A potent inhibitor of Aurora A kinase (IC50 = 42 nM); selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively)
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Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
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A cell-permeable inhibitor of MMPs that most potently inhibits MMP-9 and MMP-13 (IC50s = 0.9 nM for both); less effectively inhibits MMP-1, MMP-3, and MMP-7 (IC50s = 43, 23, and 920 nM, respectively)
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An IMP1 inhibitor (IC50 = 5 μM for IMP1 binding to c-Myc mRNA); downregulates c-Myc and β-TrCP1 mRNA and reduces IMP1 protein levels in SK-MEL-2 and IGROV-1 cells; inhibits proliferation of IMP1-positive ES-2, IGROV-1, and SK-MEL-2 cells (IC50s = 2.3, 3.6, and 4.5 μM, respectively); inhibits anchorage-independent growth of SK-MEL-2 cells at 10 μM
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An inhibitor of PI4KIIIβ (IC50 = 19 nM); ~100-fold selective for PI4KIIIβ over PI4KIIα, PI4KIIβ, and PI4KIIIα, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, and PI3KC3, as well as 100-500-fold selective over PI3KC2α, PI3KC2β, and PI3KC2γ
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MW 696.8 Da, Purity >98%. Specific inhibitor of the lysine-specific methyltransferase SU (VAR)3-9 both in vitro and in vivo. It displays potent antimyeloma activity in IL-6-dependent myeloma cell lines. Its antimyeloma activity appears to be due to induction of oxidative stress and consequent apoptosis.
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Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFR?, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 ?M. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 ?M. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS). *For Research & Development use only. Product is not intended for drug, household, or human consumption.
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