IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). 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.
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- CAS No.: 686772-17-8
- Formule: C23H20N4O3S3
- Masse moléculaire:496.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CK1δ 1.06 μM (IC50) |
CK1ε 7.07 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | EC50 |
0.23 μM
Compound: IWP-4
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Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
IWP-4 (GMP) (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 (GMP) (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.
Chemical Information
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CAS No. 686772-17-8
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Masse moléculaire 496.62
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Formule C23H20N4O3S3
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SMILES
O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5OC)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018;61(9):4087-4102. [Content Brief]
[2]. Wang J, et al. A RNA-seq approach for exploring the protective effect of ginkgolide B on glutamate-induced astrocytes injury. J Ethnopharmacol. 2021;270:113807. [Content Brief]
[3].
Hudson J, et al. Primitive cardiac cells from human embryonic stem cells. Stem Cells Dev. 2012 Jun 10;21(9):1513-23.
[Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IWP-4 (GMP) Related Classifications
HY-12879G Related Classifications
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