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$0.00 - Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. Oncogenic KRAS signalling promotes the Wnt/β-catenin pathway through LRP6 in colorectal cancer, Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
Biological Activity
LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.
Targets
| Porcn (TM3 cells) | ||||
| In vitro (25°C) | DMSO | Warmed: 76 mg/mL (191.7 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+corn oil | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 25.22 mL | 126.12 mL | 252.24 mL |
| 0.5 mM | 5.04 mL | 25.22 mL | 50.45 mL |
| 1 mM | 2.52 mL | 12.61 mL | 25.22 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.04 mL |
*The above data is based on the productmolecular weight 396.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A12816 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1243244-14-5 |
| Formula | C23H20N6O |
| M. Wt | 396.44 |
| Purity | >98% |
| Synonyms | LGK974, LGK 974 |
| SMILES | CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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