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| Product Name | Tankyrase1/2 Inhibitor III |
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| Description | Purity ~99% (HPLC). A cell-permeable triazolylthiomethyl-oxadiazole compound that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (=79 and 28nM, respectively), and acts as a potent and reversible TNKS1/2 dual inhibitor (IC50=33nM TNKS2 in an auto-PARsylation assay). Shown to interact with the adenosine diphosphate linker portion of the NAD+ donor site, and display excellent selectivity over PARP1 and PARP2 activities (IC50>19uM); stabilize Axin2 levels (EC50=709nM in SW480 cells), and antagonize Wnt signaling (IC50=215nM in HEK293-SuperTopFlash assay). Exhibits minimal activity towards cytochrome P450 enzymes (IC50=21 and 5.7uM for CYP2C9 and CYP3A4) and hERG ion channel (IC50>30uM), and adequate microsomal stability. Formula: C20H19N5O3S Molecular Weight: 409.5 Solubility: DMSO (100mg/ml) |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | Tankyrase1/2 Inhibitor III (TNKS1/2 Inhibitor III, Wnt Pathway Inhibitor XIV, 3-(4-Methoxyphenyl)-5-((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-ylthio)methyl)-1,2,4-oxadiazole) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217827 |
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| Order / More Info | Tankyrase1/2 Inhibitor III from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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