IWP-2, Porcupine (Wnt) Inhibitor

IWP-2 is a potent and highly selective Wnt signaling antagonist with an IC50 ~ 27 nM in the L-Wnt-STF cellular assay. It prevents palmitoylation of Wnt proteins by Porcupine (a membrane-bound O-acyltransferase), thereby blocking Wnt protein secretion and activity. It blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. IWP-2 is a useful chemical probe in both regenerative medicine and anticancer efforts.

Product information

CAS Number: 686770-61-6

Molecular Weight: 466.60

Formula: C22H18N4O2S3

Chemical Name: N-(6-methylbenzo[d]thiazol-2-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide

Smiles: CC1=CC2SC(NC(=O)CSC3=NC4CCSC=4C(=O)N3C3C=CC=CC=3)=NC=2C=C1

InChiKey: WRKPZSMRWPJJDH-UHFFFAOYSA-N

InChi: InChI=1S/C22H18N4O2S3/c1-13-7-8-15-17(11-13)31-21(23-15)25-18(27)12-30-22-24-16-9-10-29-19(16)20(28)26(22)14-5-3-2-4-6-14/h2-8,11H,9-10,12H2,1H3,(H,23,25,27)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 10 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

IWP-2 was used at 1-2 µM in vitro and in cellular assays.

References:

1. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. (2009) Nat Chem Biol. 5(2):100-7.
2. ten Berge D, et al. Embryonic stem cells require Wnt proteins to prevent differentiation to epiblast stem cells. (2011) Nat Cell Biol. 13(9):1070-5.
3. Lian X, et al. Robust cardiomyocyte differentiation from human pluripotent stem cells via temporal modulation of canonical Wnt signaling. (2012) Proc Natl Acad Sci USA. 109(27):E1848-57.

Products are for research use only. Not for human use.