Name: IWP-2
Brand: Selleck Chemicals
SKU: S7085
Rating: 5 (94 reviews)

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

CAS: 686770-61-6

Selleck's IWP-2 has been cited by 94 publications

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

Related Targets	WNT β-catenin Wnt/β-catenin	Click to Expand
Related Products	IWR-1-endo SKL2001 BML-284 (Wnt agonist 1) PRI-724 Salinomycin (from Streptomyces albus) FH535 PNU-74654 LF3 KYA1797K KY02111 iCRT3 Adavivint (SM04690) MSAB Isoquercitrin IQ-1 iCRT14 CCT251545 Isoxazole 9 (ISX-9) JW55 M435-1279 WAY-262611 JW74	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	Click to Expand

Signaling Pathway

Wnt/beta-catenin Signaling Pathway

Choose Selective Wnt/beta-catenin Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Experimental Result Images	Western blot	Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin MMP7		27119499

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMF : 12.5 mg/mL

DMSO : Insoluble ( 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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