IWP-2

Catalog No.S7085 Batch:S708504

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Technical Data

Formula

C22H18N4O2S3

Molecular Weight 466.6 CAS No. 686770-61-6
Solubility (25°C)* In vitro DMF 12.5 mg/mL (26.78 mM)
DMSO 10 mg/mL (21.43 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.
Targets
Wnt [1]
(Cell-free assay)
M82FCK1δ [3]
(Cell-free assay)
27 nM 40 nM
In vitro

IWP-2 is useful in both regenerative medicine and anticancer efforts. IWP-2 inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. IWP-2 blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. [1]

Features Selective inhibitor of Porcn-mediated Wnt secretion.

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    L-Wnt-STF cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    L-Wnt-STF cells that exhibit constitutive Wnt pathway activation were incubated with IWR (10μM) and IWP (5μM) compounds for 24 hrs prior to lysis. Cellular lysates were subjected to Western blot analysis.

Animal Study:

[2]

  • Animal Models

    Crl:CD1 (ICR) and FVB/N female mice

  • Dosages

    50 µg

  • Administration

    s.c.

References

  • https://pubmed.ncbi.nlm.nih.gov/19125156/
  • https://pubmed.ncbi.nlm.nih.gov/25536657/
  • https://pubmed.ncbi.nlm.nih.gov/29630366/

Customer Product Validation

KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). *P < 0.05; **P < 0.01.

Data from [ , , Sci Rep, 2016, 6:32770. ]

(b-d) Combined and temporal treatment with IWP-2, SAG and FGF8 resulted in robust induction of MGE cells from H9 and H7 hESCs as well as iPSCs, assayed after 25 days of differentiation. The image in the insets is Hoechst-labeled nuclei of the same microscope field. Scale bar: 100 μm.

Data from [ , , Methods, 2016, 101:103-12. ]

H. IWP-2, an inhibitor of Wnt signaling, rescued the cell growth in A549 cells which were co-transfected with miR-520e and pcDNA-Zbtb7a.

Data from [ , , Biochem Biophys Res Commun, 2017, 486(1):49-56 ]

Selleck's IWP-2 Has Been Cited by 146 Publications

Persistent Wnt signaling affects IVF embryo implantation and offspring metabolism [ Sci Bull (Beijing), 2025, S2095-9273(25)00472-4] PubMed: 40441968
ETVs dictate hPSC differentiation by tuning biophysical properties [ Nat Commun, 2025, 16(1):1999] PubMed: 40011454
Deciphering signaling mechanisms and developmental dynamics in extraembryonic mesoderm specification from hESCs [ Nat Commun, 2025, 16(1):4688] PubMed: 40399284
AAV vectors trigger DNA damage response-dependent pro-inflammatory signalling in human iPSC-derived CNS models and mouse brain [ Nat Commun, 2025, 16(1):3694] PubMed: 40251179
Bioimpedance and electrophysiology measurements of engineered heart tissues outside the culture medium [ Biosens Bioelectron, 2025, 287:117634] PubMed: 40614400
Allelic bias contributes to heterogeneous phenotypes of NK cell deficiency [ Cell Rep, 2025, 44(8):116102] PubMed: 40768335
The balance between IFN-γ and ERK/MAPK signaling activities ensures lifelong maintenance of intestinal stem cells [ Cell Rep, 2025, S2211-1247(25)00057-9] PubMed: 39952238
Directed and efficient generation of calretinin interneurons from human pluripotent stem cells [ Stem Cell Res Ther, 2025, 16(1):465] PubMed: 40867008
Human epicardial organoids from pluripotent stem cells resemble fetal stage with potential cardiomyocyte- transdifferentiation [ Cell Biosci, 2025, 15(1):4] PubMed: 39825425
Heightened sensitivity to adverse effects of metformin in mtDNA mutant patient cells [ Life Sci, 2025, 366-367:123486] PubMed: 39978587

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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