IWP-3 (Synonyms: Inhibitor of Wnt Production-3) |
| رقم الكتالوجGC17071 |
IWP-3 هو مثبط قوي لإنتاج Wnt مع IC 50 من 40 نانومتريثبط IWP-3 وظيفة Porcupine (Porcn) وبالتالي يمنع تكوين النخلة لبروتينات WntIWP-3 يثبط CK1γ3 و CK1ε بشكل معتدل ولا يمنع CK1α
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Cas No.: 687561-60-0
Sample solution is provided at 25 µL, 10mM.
IC50: 40 nM
IWP-3 is an inhibitor of Wnt production.
Wnt signaling proteins, a group of small secreted proteins, are active in tissue homeostasis, embryonic development, as well as tumorigenesis. Wnt proteins can bind to the cell surface receptors, initiating a signaling cascade that results in the β-catenin activation of gene transcription.
In vitro: In previous study, IWP-3 was identified as an inhibitor of Wnt production that could regulate in vitro Wnt pathway activity with an IC50 value of 40 nM. In addition, IWP-3 was found to be able to inactivate porcupine, a O-acyltransferase for palmitoylating Wnt proteins that was critical for the signaling ability and secretion. Moreover, IWP-3 at 5 μM was found to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 and the scaffold protein Dishevelled, resulting in preventing the accumulation of β-catenin [1]. In another study, IWP-3 was applied to promote cardiomyocyte generation from human embryonic stem cells by inhibiting Wnt signaling [2].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, IWP-3 is still in the preclinical development stage.
References:
[1] B. Chen, M. E. Dodge, W. Tang, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5(2), 100-107 (2009).
[2] E. Willems, S. Spiering, H. Davidovics, et al. Small molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell derived mesoderm. Circulation Research 109(4), 360-364 (2011).
| Cas No. | 687561-60-0 | SDF | |
| المرادفات | Inhibitor of Wnt Production-3 | ||
| Chemical Name | 2-[[3-(4-fluorophenyl)-3,4,6,7-tetrahydro-4-oxothieno[3,2-d]pyrimidin-2-yl]thio]-N-(6-methyl-2-benzothiazolyl)-acetamide | ||
| Canonical SMILES | O=C(CSC(N1C2=CC=C(F)C=C2)=NC3=C(SCC3)C1=O)NC4=NC5=C(C=C(C)C=C5)S4 | ||
| Formula | C22H17FN4O2S3 | M.Wt | 484.6 |
| الذوبان | ≤0.1mg/ml in DMSO;2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0636 mL | 10.3178 mL | 20.6356 mL |
| 5 mM | 412.7 μL | 2.0636 mL | 4.1271 mL |
| 10 mM | 206.4 μL | 1.0318 mL | 2.0636 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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