Purvalanol A

SKU: orb1225673

Description

A potent, cell-permeable, selective inhibitor of CDK with IC50s of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively; also inhibits Saccharomyces cerevisiae Cdc28p (IC50=80 nM) and has no effect on PKC, Raf, CK1, CK2.

Key Properties

• CAS Number: 212844-53-6
• MW: 388.8944
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₅ClN₆O
• SMILES: CC(C)[C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO
• Target: CDK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  Purvalanol A inhibits cdc28 (S. cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of 76 nM and the NCI-H522 non-small cell lung cancer cell line with a GI50 of 347 nM. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26, 84 μM. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions.

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

NG-60 | NG 60 | NG60

Quick Database Links

Gene Symbol

CDK