All AbMole products are for research use only, cannot be used for human consumption.
ETC-159 is a potent, selective and orally available PORCN inhibitor, which inhibits β-catenin reporter activity with an IC50 of 2.9 nM. ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models driven by high Wnt signaling.
ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately four fold higher (70 nM). ETC-159 exhibits good oral pharmacokinetics in mice allowing preclinical evaluation via oral administration. After a single oral dose of 5 mg/kg, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells, STF3A cells |
| Preparation method | HEK293 cells stably transfected with STF reporter and pPGK-WNT3A plasmid (STF3A cells) are treated with varying concentrations of compounds. For Wnt secretion, STF3A cells are treated with ETC-159 diluted in 1% fetal bovine serum-containing media. |
| Concentrations | 100 nm |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | Formulated in 50% PEG400 (vol/vol) in water |
| Dosages | 10 μL/g |
| Administration | oral gavage |
| Molecular Weight | 391.38 |
| Formula | C19H17N7O3 |
| CAS Number | 1638250-96-0 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Wnt/beta-catenin Products |
|---|
| (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide
(9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide is a macamide isolated from Maca (Lepidium meyenii Walp). (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide induces mesenchymal stem cells osteogenic differentiation and consequent bone formation through activating the canonical Wnt/β‐catenin signaling pathway. |
| F7H
F7H is a Frizzled receptor FZD7 antagonist with IC50 of 1.25 μM. F7H is a potent ligand for the FZD7 transmembrane domain (TMD). |
| UU-T02
UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction, with a Ki of 1.36 μM. UU-T02 inhibits canonical Wnt signaling. |
| Wnt/β-catenin agonist 1
Wnt/β-catenin agonist 1 is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM. |
| Calphostin C
Calphostin C (PKF115-584) is a small molecule inhibitor of Wnt/beta-catenin/lef-1 signaling. Calphostin C is also a potent and specific inhibitor of protein kinase C. PKF115-584 efficiently killed CLL cells (LC(50)<1 microM), whereas normal B cells were not significantly affected. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
