KenPaullone

SKU: orb1305901

Description

Kenpaullone (9-Bromopaullone) is a potent CDK1/2/5 inhibitor that promotes induced regulatory T (iTreg) cell differentiation via enhanced TGFβ-Smad3 signaling and sustained foxp3 transcription. It is applied in immunology research, including autoimmune disease and cancer immunotherapy studies, utilizing both in vitro and in vivo experimental models.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 142273-20-9
• MW: 327.18
• Purity: 97.92%
• Formula: C₁₆H₁₁BrN₂O
• SMILES: Brc1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1
• Target: GSK-3,CDK
• Solubility: DMSO:41.67 mg/mL (127.36 mM);Ethanol:1.6 mg/mL (4.89 mM)

Bioactivity

• Target IC50:
  CDK2-CyclinA:0.6 μM|CDK2-CyclinE:7. μM|ERK1:20 μM|C-Raf:38 μM|CDK1-CyclinB:0. μM|GSK-3β:0.2 μM|CDK5-p35:0.8 μM|ERK2:9 μM
• In Vitro:
  In HEK-293 cells, phosphorylation o the endogenous GSK3α on Tyr279 is greatly decreased after prolonged incubation with Kenpaullone. Also the Phosphorylation o the endogenous GSK3β also decreases, although less markedly. Kenpaullone also induce the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. Kenpaullone (20 μM) strongly suppresse the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. col [2.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

CDK, CDK1/CyclinB, CDK2/CyclinA, CDK2/CyclinE, CDK5/p35, Cyclin dependent kinase, 9-Bromopaullone, KenPaullone, inhibit, NSC664704, NSC-664704, NSC 664704, Inhibitor, Glycogen synthase kinase-3, Glycogen synthase kinase 3, GSK-3, GSK3, GSK-3β

Compound Identifiers

PubChem CID

3820