SKL2001 是一种Wnt/β-CATenin信号通路的激动剂，具有抗肿瘤作用。它能够破坏 Axin/β-CATenin 相互作用，稳定细胞内 β-CATenin。

SKL2001, an agonist of the Wnt/β-catenin pathway, can disrupt the Axin/β-catenin interaction.

SKL2001 upregulated β-catenin responsive transcription by increasing the intracellular β-catenin protein level and inhibited the phosphorylation of β-catenin at residues Ser33/37/Thr41 and Ser45, which would mark it for proteasomal degradation, without affecting CK1 and GSK-3β enzyme activities. SKL2001 disrupted the Axin/β-catenin interaction, which is a critical step for CK1- and GSK-3β-mediated phosphorylation of β-catenin at Ser33/37/Thr41 and Ser45. The treatment of mesenchymal stem cells with SKL2001 promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. SKL2001 did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity[1].

The HEK293 reporter and control cell lines were established. The HEK293 reporter cells were inoculated into 384-well plates at 10 000 cells per well and grown for 24 h. Next, each compound in the chemical library (～270 000) was added to at a final concentration of 20 μM. After 15 h, the plates were assayed for firefly luciferase activity.(Only for Reference)

909089-13-0

C14H14N4O3

286.291

Ethanol:53 mg/mL (185.1 mM)
H2O:<1 mgml
DMSO:53 mg/mL (185.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years