SKL2001

SKU: orb1223681

Description

SKL2001 is a specific small molecule activator (agonist) of the Wnt/β-catenin pathway, stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction; strongly activates β-catenin responsive transcription, upregulates TOPflash reporter activity without effect on the activity of FOPFlash with mutated β-catenin/Tcf-binding elements, as well as either NF-κB or p53 reporter activity; upregulates the expression of Axin2, inhibits N-terminal β-catenin phosphorylation without affecting GSK-3β activity; suppresses preadipocyte differentiation, the alternative mesenchymal differentiation pathway.(In Vitro):SKL2001 is an agonist of the Wnt/β-catenin pathway, and also upregulates the expression of Axin2, a downstream target of the Wnt/β-catenin pathway, but shows no effect on NF-κB, p53 reporter activity and GSK-3β activity. SKL2001 causes osteoblast differentiation (20 and 40 μM) and suppresses preadipocyte differentiation (5, 10, and 30 μM) via the activation of the Wnt/β-catenin pathway. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible; SKL2001 cuases cell cycle arrest in HCT116 spheroids. SKL2001 (40 μM) enhances round-shape spheroid formation and E-cadherin expression.

Key Properties

• CAS Number: 909089-13-0
• MW: 286.291
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₄N₄O₃
• SMILES: O=C(C1=NOC(C2=CC=CO2)=C1)NCCCN3C=CN=C3
• Target: Beta-catenin
• Solubility: DMSO: 53 mg/mL (185.1 mM); Ethanol: 53 mg/mL (185.1 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  SKL2001 is an agonist of the Wnt/β-catenin pathway, and also upregulates the expression of Axin2, a downstream target of the Wnt/β-catenin pathway, but shows no effect on NF-κB, p53 reporter activity and GSK-3β activity. SKL2001 causes osteoblast differentiation (20 and 40 μM) and suppresses preadipocyte differentiation (5, 10, and 30 μM) via the activation of the Wnt/β-catenin pathway. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible; SKL2001 cuases cell cycle arrest in HCT116 spheroids. SKL2001 (40 μM) enhances round-shape spheroid formation and E-cadherin expression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SKL 2001 | SKL-2001

Quick Database Links

Gene Symbol

Beta-catenin