1-Azakenpaullone

SKU: orb1300838

Description

1-Azakenpaullone

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 676596-65-9
• MW: 328.16
• Purity: 99.73%
• Formula: C₁₅H₁₀BrN₃O
• SMILES: Brc1ccc2[nH]c-3c(CC(=O)Nc4cccnc-34)c2c1
• Target: GSK-3
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (182.84 mM)

Bioactivity

• Target IC50:
  CDK5-p25:4.2 μM|GSK-3β:18 nM|CDK1-CyclinB:2 μM
• In Vivo:
  Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive de cits, and improves the ketamine-induced motor incoordination in rotarod test.
• In Vitro:
  1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death.
• Cell Research:
  Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. The relative cell number is determined after treatment with 1-Azakenpaullone for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, GSK-3β, Glycogen synthase kinase 3, Glycogen synthase kinase-3, GSK-3, GSK3, Inhibitor, 1Azakenpaullone, 1-Azakenpaullone, 1-Akp, 1 Azakenpaullone, azakenpaullone

Compound Identifiers

PubChem CID

6538897