531091 Sigma-AldrichPorcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem
A cell-permeable inhibitor of Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC₅₀ from 50 pM to 1.1 nM).
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Synonymes: 2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974
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Aperçu
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Tableau de caractéristiques principal
| CAS # | Empirical Formula |
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| 1243244-14-5 | C₂₃H₂₀N₆O |
Products
| Référence | Conditionnement | Qté | |
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| 5310910001 | Flacon en verre | 5 mg |
| Description | |
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| Overview | A cell-permeable C59 (Cat. No. 500496) structural analog that potently inhibits Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC50 from 50 pM to 1.1 nM) via direct porcupine (Porcn), but not Wntless, affinity interaction. Shown to inhibit the proliferation of head and neck squamous cell carcinoma (HNSCC) line HN30 (IC50 = 0.3 nM), but not 293T even at a high concentration of 20 µM. In mice & rats receiving therapeutic LGK974 oral dosages (up to 5 mg/10 mL/kg/d), a delayed tissue Wnt signaling suppression (max inhibition 7 to 10 h post dosing) is seen due to pre-existing Wnt in tissue, followed by a full recovery of tissue Wnt signalling at 24 h upon drug clearance. The periodic daily inhibition/recovering cycle is shown to result in tumor regression in mice & rats, while allowing Wnt signaling-dependent normal tissue homeostasis. Overdosing is reported to result in loss of intestinal epithelium in rats receiving 14 consecutive 20 mg/kg daily oral dosages. |
| Catalogue Number | 531091 |
| Brand Family | Calbiochem® |
| Synonyms | 2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974 |
| References | |
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| References | Liu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224. |
| Product Information | |
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| CAS number | 1243244-14-5 |
| Form | Tan powder |
| Hill Formula | C₂₃H₂₀N₆O |
| Chemical formula | C₂₃H₂₀N₆O |
| Reversible | Y |
| Quality Level | MQ100 |
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| Biological Information | |
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| Primary Target | Porcupine |
| Purity | ≥97% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Référence | GTIN |
| 5310910001 | 04055977242614 |
Documentation
Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem FDS
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Références bibliographiques
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| Liu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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