IWR-1-endo
IWR-1-endo is a small molecule inhibitor of Wnt Response with IC50 value of 180nM [1].
IWR-1-endo is a small molecule antagonists of the Wnt/β-catenin pathway screened out from a diverse synthetic chemical library. It acts as an inhibitor of Wnt response. IWR-1-endo can inhibit the activity of Wnt1, 2 and 3. In cultured cells, IWR-1-endo inhibits Wnt-induced β-catenin accumulation which is a downstream event of Lrp6 and Dvl2. It is proved that IWR-1-endo promote β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo is also shown to inhibit tailfin regeneration and epithelial stem cell self-renewal in zebrafish. These two processes are both dependent on Wnt/β-catenin signaling. Furthermore, IWR-1-endo can block aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss [1].
References:
[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
- 1. Qi Zhu, Dinghui Wang, et al. "Protein arginine methyltransferase PRMT1 promotes adipogenesis by modulating transcription factors C/EBPβ and PPARγ." J Biol Chem. 2022 Jul 31;102309. PMID: 35921899
- 2. Yang H, Li G, et al. "Secreted frizzled-related protein 2 promotes the osteo/odontogenic differentiation and paracrine potentials of stem cells from apical papilla under inflammation and hypoxia conditions." Cell Prolif. 2019 Sep 30:e12694. PMID: 31568642
- 3. Suknuntha K, Tao L, et al. "Optimization of Synthetic mRNA for Highly Efficient Translation and its Application in the Generation of Endothelial and Hematopoietic Cells from Human and Primate Pluripotent Stem Cells." Stem Cell Rev. 2018 Mar 8. PMID: 29520567
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 409.44 |
| Cas No. | 1127442-82-3 |
| Formula | C25H19N3O3 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥20.45 mg/mL in DMSO |
| Chemical Name | 4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)-N-(quinolin-8-yl)benzamide |
| SDF | Download SDF |
| Canonical SMILES | O=C([C@@]1([H])[C@]2([H])[C@]3([H])C([H])([H])[C@@]1([H])C([H])=C3[H])N(C4=C([H])C([H])=C(C(N([H])C5=C([H])C([H])=C([H])C6=C5N=C([H])C([H])=C6[H])=O)C([H])=C4[H])C2=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
DLD-1 colorectal cancer (CRC) cell line |
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Preparation method |
The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 μM, 2.5 μM, 10 μM |
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Applications |
IWR-1-endo promoted β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo blocked aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss. |
| Animal experiment [1]: | |
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Animal models |
Zebrafish |
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Dosage form |
10 mM, 24 h |
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Application |
IWR-1-endo inhibited tailfin regeneration and epithelial stem cell self-renewal in zebrafish. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. |
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| Description | IWR-1-endo is a potent inhibitor of Wnt signaling with IC50 value of 180 nM. | |||||
| Targets | Wnt signaling | |||||
| IC50 | 180 nM | |||||
Quality Control & MSDS
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Chemical structure
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