IWR-1,5MG,50446200011753,Sigma

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订货号 0BV5496
品牌型号 Sigma 50446200011753
货期 询货期
最小订货量 1件
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产品介绍 Product Description

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
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.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Irritant (B)


技术参数 Specifications
Quality Segment100
assay≥95% (HPLC)
formliquid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,avoid repeated freeze/thaw cycles,desiccated (hygroscopic),protect from light
storage temp.−70°C
SMILES stringN4(C(=O)[C@@H]5[C@@H]([C@H]6C[C@@H]5C=C6)C4=O)c1ccc(cc1)C(=O)Nc2c3ncccc3ccc2
InChI1S/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 keyZGSXEXBYLJIOGF-ALFLXDJESA-N
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