SKL2001

SKU: orb1300283

Description

SKL2001 is a small molecule Wnt/β-catenin pathway agonist that functions by disrupting the Axin/β-catenin interaction. This tool compound is used in both in vitro and in vivo research to investigate Wnt signaling in stem cell biology, oncology, and regenerative medicine.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 909089-13-0
• MW: 286.9
• Purity: >98%
• Formula: C₁₄H₁₄N₄O₃
• SMILES: O=C(NCCCn1ccnc1)c1cc(on1)-c1ccco1
• Target: Transcription factor
• Solubility: Soluble in DMSO (at least 25 mg/ml)

Bioactivity

• In Vitro:
  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.
• Cell Research:
  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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

bcatenin, Beta catenin, betacatenin, beta-catenin, inhibit, Inhibitor, β-catenin, βcatenin, SKL 2001, SKL2001, SKL-2001, Wnt/betacatenin, Wnt/β-catenin, Wnt, Wnt/b-catenin

Compound Identifiers

PubChem CID

16003447