IWP 2

Tocris Bioscience | Catalog # 3533

PORCN inhibitor; inhibits Wnt processing and secretion
Tocris Bioscience

Key Product Details

Description

PORCN inhibitor; inhibits Wnt processing and secretion
View all PORCN Inhibitors »

Product Description

IWP 2 is a potent inhibitor of Wnt processing and secretion (IC50 = 27nM). IWP 2 inactivates PORCN, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. Blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. IWP 2 suppresses self-renewal in R1 embryonic stem cells and promotes cardiomyocyte differentiation from hPSCs. The compound has also been used in protocols to reprogram human somatic cells to chemically-induced PSCs.

Scientific Data Images for IWP 2

iPSC-derived heart organoids differentiated with IWP 2 and CHIR 99021

iPSC-derived Human Heart-forming Organoids

Human iPSCs were embedded in Cultrex™ UltiMatrix RGF Basement Membrane Extract (R&D Systems, Catalog # BME001-05) and differentiated with CHIR 99021 (Tocris Bioscience, Catalog # TB4423-GMP) and IWP 2 (Tocris Bioscience, Catalog # 3533) into heart-forming organoids based on a protocol from Drakhlis, L. et al. (2021) Nat. Biotechnol. 39:737. Successful differentiation was demonstrated by staining the cells with A) a Rabbit Anti-Human Cardiac Troponin T Antigen Affinity-purified Polyclonal Antibody (green; Novus Biologicals, Catalog # NBP3-13391) to detect cardiomyocytes and a Goat Anti-Human CD31/PECAM-1 Antigen Affinity-purified Polyclonal Antibody (red; R&D Systems, Catalog # AF3628) to detect endothelial cells. The cells were counterstained with DAPI (blue; Tocris Bioscience, Catalog # 5748). As formation of early embryonic heart anlagen is associated with nascent foregut endoderm development, cells were also stained with B) a Goat Anti-Human SOX2 Antigen Affinity-purified Polyclonal Antibody (red; R&D Systems, Catalog # AF2018) and a Mouse Anti-Human HNF-4 alpha/NR2A1 Monoclonal Antibody (green; R&D Systems, Catalog # PP-K9218-00) to detect anterior and posterior foregut endoderm cells, respectively. The cells were counterstained with DAPI (blue; Tocris Bioscience, Catalog # 5748).

Product Specifications for IWP 2

Molecular Weight

466.60

Formula

C22H18N4O2S3

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide

CAS Number

686770-61-6

PubChem ID

2155128

InChI Key

WRKPZSMRWPJJDH-UHFFFAOYSA-N

SMILES

O=C1C3=C(CCS3)N=C(SCC(NC4=NC(C=CC(C)=C5)=C5S4)=O)N1C2=CC=CC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.33 5 with gentle warming

Preparing Stock Solutions for IWP 2

The following data is based on the product molecular weight 466.60.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 42.86 mL 214.32 mL 428.63 mL
0.25 mM 8.57 mL 42.86 mL 85.73 mL
0.5 mM 4.29 mL 21.43 mL 42.86 mL
2.5 mM 0.86 mL 4.29 mL 8.57 mL

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 503 publications citing the usage of this product.

Product Documents for IWP 2

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for IWP 2

For research use only

Customer Reviews for IWP 2 (3)

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Customer Images

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  • IWP2 for small molecule pathway
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Verified Customer | Posted 07/23/2021
    IWP2 was used for cardiomyocyte differentiation of pluripotent stem cells. IWP2 was used at a concentration of 5 uM on day 3 of the differentiation schedule. The image shows differentiated cardiomyocytes.
    IWP 2 3533
  • Wnt pathway inhibitor that works really well
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Verified Customer | Posted 12/09/2019
    I used it as a Wnt pathway inhibitor in Hepatocellular Carcinoma Cells. I used the concentration 5uM and it works really well.
  • IWP2 for cardiac differentiation.
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Cell Line/Tissue: human foreskin fibroblasts-derived-IPS
    Verified Customer | Posted 02/01/2018
    I use it as a blocking molecule of the WNT pathway for cardiac differentiation in foreskin fibroblast-derive IPS cells. I obtained succesfully cardiomyocytes in a 5uM concentration.
    IWP 2 3533

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