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Tankyrase1/2 Inhibitor III
3-(4-Methoxyphenyl)-5-((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-ylthio)methyl)-1,2,4-oxadiazole, TNKS1/2 Inhibitor III, Wnt Pathway Inhibitor XIV
A cell-permeable triazolylthiomethyl-oxadiazole compound that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (Kd = 79 and 28 nM, respectively), and acts as a potent and reversible TNKS1/2 dual inhibitor (IC50 = 33 nM 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 > 19 µM); stabilize Axin2 levels (EC50 = 709 nM in SW480 cells), and antagonize Wnt signaling (IC50 = 215 nM in HEK293-SuperTopFlash assay). Exhibits minimal activity towards cytochrome P450 enzymes (IC50 = 21 and 5.7 µM for CYP2C9 and CYP3A4) and hERG ion channel (IC50 > 30 µM), and adequate microsomal stability.
产品信息
Form White solid
Primary Target TNKS1/PARP5a and TNKS2/PARP5b
Molar mass 409.5
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Reversible 是的
Purity ≥99% by HPLC
Solubility DMSO
CAS number 865565-29-4
商店和运输信息
Storage +2°C to +8°C
Ship Ambient or Dry Ice
Standard Handling |