1. Stem Cell/Wnt Cell Cycle/DNA Damage
  2. Wnt Casein Kinase
  3. IWP-4

IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.

For research use only. We do not sell to patients.

IWP-4

IWP-4 Chemical Structure

CAS No. : 686772-17-8

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of IWP-4:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure[1][2][3].

IC50 & Target

IC50: 25 nM (Wnt)[1]

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 EC50
0.23 μM
Compound: IWP-4
Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
[PMID: 29630366]
HEK293 EC50
0.28 μM
Compound: IWP-4
Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
[PMID: 29630366]
HT-29 EC50
0.34 μM
Compound: IWP-4
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
[PMID: 29630366]
MIA PaCa-2 EC50
0.23 μM
Compound: IWP-4
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
[PMID: 29630366]
PANC-1 EC50
0.23 μM
Compound: IWP-4
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
[PMID: 29630366]
SW-620 EC50
0.23 μM
Compound: IWP-4
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
[PMID: 29630366]
In Vitro

IWP-4 (48 h) inhibits the proliferation of all tested cancer cell lines, with submicromolar EC50 values ranging from 0.23 μM to 0.93 μM[1].
IWP-4 (1 μM; 24 h) antagonizes the protective effect of Ginkgolide B (HY-N0784) on primary rat cortical astrocytes against glutamate-induced injury by reversing Ginkgolide B-mediated regulation of apoptosis-related genes and proteins, as well as glutamate transporter genes and proteins[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

496.62

Formula

C23H20N4O3S3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 1.72 mg/mL (3.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0136 mL 10.0681 mL 20.1361 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

References
Cell Assay
[1]

hESC cultures are obtained in mTeSR-1 medium and expanded with daily medium exchange until colonies reach the desired level of confluence (~70% to 80%). At this time (marked day 0), mTeSR-1 is replaced with a basal medium comprised of RPMI 1640 medium supplemented with 2% B27 supplement and 1% penicillin/streptomycin. 20 ng/mL BMP-4 and/or 6 ng/mL activin A are added to the basal medium for primitive streak induction, and exchanged daily until day 3. Then, basal media with or without 5 mM IWP-4 is added to the cells and exchanged every 2 days [dimethyl sulfoxide (DMSO) at the same concentration is used as a vehicle control] until day 15, after which basal medium is supplied every 2 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0136 mL 10.0681 mL 20.1361 mL 50.3403 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
IWP-4
Cat. No.:
HY-12879
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