575546
Tankyrase1/2 Inhibitor III
The Tankyrase1/2 Inhibitor III controls the biological activity of Tankyrase1/2.
别名:
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, 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
InChI key
LQZSHPITKSPDLC-UHFFFAOYSA-N
InChI
1S/C20H19N5O3S/c1-13-22-23-20(25(13)15-6-10-17(27-3)11-7-15)29-12-18-21-19(24-28-18)14-4-8-16(26-2)9-5-14/h4-11H,12H2,1-3H3
SMILES string
CC1=NN=C(SCC2=NC(C3=CC=C(C=C3)OC)=NO2)N1C(C=C4)=CC=C4OC
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
TNKS1/PARP5a and TNKS2/PARP5b
TNKS1/PARP5a and TNKS2/PARP5b
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Avoid freeze/thaw cycles of solutions.
Other Notes
Shultz, M.D., et al. 2012. J. Med. Chem.55, 1127.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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