Alsteropaullone

SKU: orb1225556

Description

Alsteropaullone (9-Nitropaullone, NSC 705701) is a derivative of kenpaullone, ATP-competitive inhibitor of CDKs and GSK3β, inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E and Cdk5/p25 with IC50 of 35, 15, 200 and 40 nM; exhibits specific antitumor activity against Group 3 medulloblastomas, causes inhibition of cell cycle-related genes, and down-regulation of MYC; inhibits the cytosolic degradation of β-catenin to alter the canonical Wnt signaling pathway in primary axis patterning, reduces tau phosphorylation.

Key Properties

• CAS Number: 237430-03-4
• MW: 293.3
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₁N₃O₃
• SMILES: O=C1NC2=CC=CC=C2C(NC3=C4C=C([N+]([O-])=O)C=C3)=C4C1
• Target: CDK

Bioactivity

• In Vivo:
  Alsterpaullone (30 mg/kg, s. c. , daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts. Animal model: 5-6 week old athymic nude mice. Dosage: 30 mg/kg. Administration: Subcutaneous injections, daily for 2 weeks. Result: Antitumor effect in Group 3 medulloblastomas.
• In Vitro:
  Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line. Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too. Alsterpaullone (20 μM) induces cell death depending on caspase activity. Cell Viability Assay Cell line: HeLa cells. Concentration: 5, 10, 15, 20, 25, 30 μM. Incubation time: 48 and 72 hours. Result: The growth of HeLa cells was inhibited in a dose-dependent manner for 48 h and 72 h ranging from 0 to 30 μM. Apoptosis Analysis Cell line: Jurkat cell line. Concentration: 0.3, 1, 3 μM Incubation time: 8 hours. Result: Induced dose-dependent apoptosis. 1 μM was sufficient to cause apoptosis, 3 μM demonstrated maximal apoptotic effects. Western blot analysis. Cell line: HeLa cells. Concentration: 2, 4, 6, 12, 24 hours. Incubation time: 8 hours. Result: The cleavage of PARP started at 4 h, while the activation of caspase-3 occurred at 2 h.

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

9-Nitropaullone | NSC 705701

Quick Database Links

Gene Symbol

CDK