Purvalanol A

SKU: orb1306602

Description

Purvalanol A (NG-60) is a potent, cell-permeable inhibitor of cyclin-dependent kinases (CDKs). It demonstrates high selectivity with IC50 values of 70, 4, 35, and 850 nM for cdk2/cyclin A, B, E, and cdk4/cyclin D1, respectively. This compound is widely used in vitro to study cell cycle regulation, apoptosis, and oncogenesis.

Research Area

Cell Biology, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 212844-53-6
• MW: 388.89
• Purity: >98%
• Formula: C₁₉H₂₅ClN₆O
• SMILES: CC(C)C(CO)Nc1nc(Nc2cccc(Cl)c2)c2ncn(C(C)C)c2n1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 35 mg/ml)

Bioactivity

• Target IC50:
  CDC2-cyclinB:4 nM|CDK2-CyclinE:35 nM|ERK1:9000 nM|CDK4-CyclinD1:850 nM|CDK2-CyclinA:70 nM|CDK5-p35:75 nM
• In Vivo:
  In MCF-7 cells, Purvalanol A leads to a 50% reduction in cell viability, while MDA-MB-231 cells exhibit lower sensitivity to Purvalanol A, showing a 32% decrease in cell viability. Purvalanol A induces mitochondrial-mediated apoptosis in both MCF-7 and MDA-MB-231 cells. The compound's effect on reducing the viability of these cell lines is dose-dependent. By inhibiting cell cycle progression and the c-Src signaling pathway, Purvalanol A effectively prevents c-Src-mediated transformation and significantly inhibits anchorage-independent growth in certain human cancer cells with upregulated c-Src. Additionally, Purvalanol A markedly suppresses anchorage-dependent growth in HT29 and SW480 human colorectal cancer cells.
• Cell Research:
  Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically.(Only for Reference)

Storage & Handling

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

Alternative Names

NG-60

Compound Identifiers

PubChem CID

4987