Chemical Structure : ETC-451
CAS No.:
2759749-82-9
ETC-451
(ETC-2188451, ETC451)
Catalog No.: PC-22869Not For Human Use, Lab Use Only.
ETC-451 (ETC-2188451) is a specific small molecule inhibitor of the Wnt transporter Wntless (WLS/Evi) with IC50 of 7.7 uM in Wnt/β-catenin reporter assays in STF3A cells, blocks the interaction of Wnt with Wntless.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ETC-451 (ETC-2188451) is a specific small molecule inhibitor of the Wnt transporter Wntless (WLS/Evi) with IC50 of 7.7 uM in Wnt/β-catenin reporter assays in STF3A cells, blocks the interaction of Wnt with Wntless.
ETC-2188451 selectively inhibits signaling in STF3A cells, but not in STF cells stimulated with WNT3A-conditioned medium, also does not block signaling resulting from downstream stimuli including activated LRP6 (ΔN-LRP6), stabilized β-catenin (β-catenin S45A mutant) and a GSK3 inhibitor BIO.
ETC-2188451 (5-50 uM) decreases WNT3A protein secretion in the culture supernatants and lysates of STF3A cells.
ETC-451 (0-40 uM) reduces Wnt target gene expression and colony formation in Wnt sensitive pancreatic cells, including AXIN2 and RNF43, also causes the upregulation of differentiation markers such as MUC.
Physicochemical Properties
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M.Wt
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346.45
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Formula
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C16H22N6OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(aminomethyl)-N-(1-(tetrahydro-2H-thiopyran-4-yl)-1H-pyrazol-3-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxamide
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References
1. Yu J, et al. iScience. 2024 Jul 5;27(8):110454.
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