Sigma-Aldrich Insolution Wnt Antagonist

Quality Level

100

Assay

≥95% (HPLC)

Form

liquid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

Storage Temp.

−70°C

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

General Description

A cell-permeablep-imidobenzamidoquinoline,endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b inin vitroauto-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-endoand XAV939 (Tankyrase1/2 Inhibitor; >Cat. No. 575545) act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects bothin vitroandin vivo, IWR-1-endoexerts its effect via interaction with Axin, while XAV939 binds TNKS directly.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
AxinReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical Form

A 25 mm (5 mg/489 µL) solution of Wnt Antagonist I, IWR-1-endo(Cat. No. 681669) in DMSO.

Reconstitution

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.Nature 461,614.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany