5.04462
IWR-1
InSolution, ≥95%, 25 mM in DMSO, Wnt Antagonist I, endo
别名:
InSolution Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I
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关于此项目
经验公式（希尔记法）:
C25H19N3O3
化学文摘社编号:
分子量:
409.44
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
form
liquid
SMILES string
N4(C(=O)[C@@H]5[C@@H]([C@H]6C[C@@H]5C=C6)C4=O)c1ccc(cc1)C(=O)Nc2c3ncccc3ccc2
InChI
1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)/t16-,17+,20-,21+
InChI key
ZGSXEXBYLJIOGF-ALFLXDJESA-N
assay
≥95% (HPLC)
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
storage temp.
−70°C
Quality Level
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General description
A cell-permeable p-imidobenzamidoquinoline, endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays (IC50 = 131 and 56 nM, respectively) and effectively suppress Wnt-stimulated transcription activity in L-Wnt-STF-based reporter assays (IC50 = 180 nM), while exhibiting little activity against PARP1 or PARP2 (IC50 >18.75 µM). Although both IWR-1-endo and XAV939 (Tankyrase1/2 Inhibitor; >Cat. No. 575545) act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1-endo exerts its effect via interaction with Axin, while XAV939 binds TNKS directly.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Axin
Axin
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 25 mM (5 mg/489 µL) solution of Wnt Antagonist I, IWR-1-endo (Cat. No. 681669) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
Other Notes
Wang, H., et al. 2011. ACS Chem. Biol.6, 192.
Chen, B., et al. 2009. Nature Chem. Biol.5, 100.
Huang, S.M., et al. 2009. Nature461, 614.
Chen, B., et al. 2009. Nature Chem. Biol.5, 100.
Huang, S.M., et al. 2009. Nature461, 614.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - (refers to pure substance)
flash_point_c
87 °C - (refers to pure substance)
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