For research use only. Not for therapeutic Use.
SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1[1].
SGC-AAK1-1 (1.25 μM) significantly reduces phosphorylation of AP2M1 (T156) and activates WNT-driven BAR activity compared in a dose-dependent manner in HT1080 cells[1].
SGC-AAK1-1 blocks AAK1 kinase activity, resulting in increased β-catenin protein stability and β-catenin-dependent transcription[1].
| Catalog Number | I017874 |
| CAS Number | 2247894-32-0 |
| Synonyms | N-[6-[3-(diethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide |
| Molecular Formula | C21H25N5O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H25N5O3S/c1-3-26(4-2)30(28,29)25-17-7-5-6-15(12-17)16-10-11-18-19(13-16)23-24-20(18)22-21(27)14-8-9-14/h5-7,10-14,25H,3-4,8-9H2,1-2H3,(H2,22,23,24,27) |
| InChIKey | UCBIQZUJJSVQHL-UHFFFAOYSA-N |
| SMILES | CCN(CC)S(=O)(=O)NC1=CC=CC(=C1)C2=CC3=C(C=C2)C(=NN3)NC(=O)C4CC4 |
| Reference | [1]. Agajanian MJ, et al. WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. Cell Rep. 2019 Jan 2;26(1):79-93.e8. |
