Home Stem Cells & Wnt Wnt/beta-catenin inhibitor - Casein Kinase inhibitor IWP-2 For research use only.

IWP-2

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.

IWP-2 Chemical Structure

IWP-2 Chemical Structure

CAS No. 686770-61-6

Purity & Quality Control

Products often used together with IWP-2

IWP-4

IWP-2 and IWP-4 are WNT inhibitors that are commonly used as small molecules for human cardiomyocytes (CMs) differentiation.

Moon SH, et al. Int J Stem Cells. 2017 May 30;10(1):1-11.

LGK-974

IWP-2 and LGK-974 decrease both sphere formation and transcriptional activities of CD44 in both RWPE-1 and PZ-HPV7 knock down (KD) cells.

Yun EJ, et al. Clin Cancer Res. 2016 Feb 1;22(3):670-9.

PRI-724

IWP-2 and PRI-724 induce apoptosis, affect HNSCC cell migration, and strongly affect β-catenin-dependent gene expression in HNSCC cells.

Kleszcz R, et al. Cell Oncol (Dordr). 2019 Aug;42(4):505-520.

IWP-2 Related Products

Signaling Pathway

Wnt/beta-catenin Signaling Pathways

Wnt/beta-catenin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse L cells Function assay 24 h Inhibition of porcupine-mediated Wnt signalling in mouse L cells after 24 hrs by SpringerImages-Topflash reporter assay, EC50=30 nM 23477365
HEK293T Function assay 22 hrs Inhibition of porcupine in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs by Super-top flash reporter gene assay, IC50 = 0.157 μM. 29630366
MIAPaCa2 Antiproliferative assay 48 hrs Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay, EC50 = 1.9 μM. 29630366
SW620 Antiproliferative assay 48 hrs Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay, EC50 = 1.9 μM. 29630366
Capan1 Antiproliferative assay 48 hrs Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay, EC50 = 2.05 μM. 29630366
PANC1 Antiproliferative assay 48 hrs Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay, EC50 = 2.33 μM. 29630366
HEK293 Antiproliferative assay 48 hrs Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, EC50 = 2.76 μM. 29630366
Panc89 Antiproliferative assay 48 hrs Antiproliferative activity against human Panc89 cells after 48 hrs by MTT assay, EC50 = 3.86 μM. 29630366
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, EC50 = 4.67 μM. 29630366
A818-6 Antiproliferative assay 48 hrs Antiproliferative activity against human A818-6 cells after 48 hrs by MTT assay, EC50 = 8.96 μM. 29630366
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Click to View More Cell Line Experimental Data

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.
Features Selective inhibitor of Porcn-mediated Wnt secretion.
Targets
Wnt [1]
(Cell-free assay)		 M82FCK1δ [3]
(Cell-free assay)
27 nM 40 nM
In vitro
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin MMP7 27119499

Chemical Information & Solubility

Molecular Weight 466.6 Formula

C22H18N4O2S3
CAS No. 686770-61-6 SDF Download IWP-2 SDF
Smiles CC1=CC2=C(C=C1)N=C(S2)NC(=O)CSC3=NC4=C(C(=O)N3C5=CC=CC=C5)SCC4
Storage (From the date of receipt)

In vitro
Batch:

DMF : 12.5 mg/mL

DMSO : 10 mg/mL ( (21.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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