IWR-1-endo A potent inhibitor of the Wnt/β-catenin response

IWR-1-endo (CAS 1127442-82-3)

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Sinónimo: 4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-benzamide
Solicitud: A potent inhibitor of the Wnt/β-catenin response
Número de CAS: 1127442-82-3
Pureza: ≥98%
Peso Molecular: 409.44
Fórmula Molecular: C25H19N3O3
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IWR-1-endo is a Wnt signaling protein, which are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and Gsk3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or Gsk3β. The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes. In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM. The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control. IWR-1-endo is an inhibitor of Tankyrase-1 and Tankyrase-2.


References

1. Polakis, P., et al., 2000. Wnt signaling and cancer. Genes & development. 14(15): 1837-51. PMID: 10921899
2. Reya, Tannishtha., et al., 2005. Wnt signalling in stem cells and cancer. Nature. 434(7035): 843-50. PMID: 15829953
3. Clevers, Hans., et al., 2006. Wnt/beta-catenin signaling in development and disease. Cell. 127(3): 469-80. PMID: 17081971
4. Chen, Baozhi., et al., 2009. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature chemical biology. 5(2): 100-7. PMID: 19125156
5. Lu, Jianming., et al., 2009. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorganic & medicinal chemistry letters. 19(14): 3825-7. PMID: 19410457

Apariencia :
Powder
Estado de Materia :
Solid
Solubilidad :
DMSO (~20 mg/mL), DMF (~20 mg/mL), and aqueous buffers (sparingly soluble).
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
310.51 °C (Predicted)
Punto de ebullición :
~643.9 °C at 760 mmHg (Predicted)
Densidad :
~1.4 g/cm3 (Predicted)
Indice de Refracción :
n20D ~1.74 (Predicted)
IC50 :
Blocking a cell-based Wnt/β-catenin pathway reporter response: IC50 = 180 nM; Beta-catenin-dependent canonical Wnt3 pathway: IC50 = 26 nM (human); Proto-oncogene protein Wnt-3: EC5050 = 5 µM (human)
Valores de pK :
pKa: 11.88 (Predicted), pKb: 2.39 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
25093485
Número MDL :
MFCD18086875
SMILES :
C1C2C=CC1[C@@H]3[C@H]2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6

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IWR-1-endo  Menciones del Producto

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Citaciones 1 a 7 de un total de 7

PMID: # 29055830  Fujita, S. et al. 2018. Bone. 106: 156-166.

PMID: # 26899563  Zhu, J. et al. 2016. Scientific reports. 6: 21549.

PMID: # 27477297  Lu, C. et al. 2016. Toxicology. 365: 35-47.

PMID: # 26048374  Mathur, R. et al. 2015. J Hematol Oncol. 8: 63.

PMID: # 25963533  Xu, Z. et al. 2015. Journal of molecular neuroscience : MN. 56: 397-408.

PMID: # 26003048  Lee, S. et al. 2015. Molecular oncology. 9: 1599-611.

PMID: # 21968810  Yasuhara, R. et al. 2011. Laboratory investigation; a journal of technical methods and pathology. 91: 1739-52.

Citaciones 1 a 7 de un total de 7
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