Purvalanol A

Catalog No.S7793

Purvalanol A Chemical Structure

Molecular Weight(MW): 388.89

Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.

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  • (A)HeLa cells were treated with Nocodazole for 8 hours and then fixed. Before the cells were stained with phospho-specific antibody against S119 of Ajuba, they were pre-incubated with PBS (no peptide control), or non-phosphorylated (control) peptide, or the phosphorylated peptide used for immunizing rabbits. CDK1 inhibitors Purvalanol A (10 μM) together with MG132 (25 μM) were added 2 h before the cells were fixed (bottom two rows).(B)Experiments were done similarly as in (A) with phospho-specific antibody against Ser175 of Ajuba.

    J Biol Chem, 2016, 291(28):14761-72.. Purvalanol A purchased from Selleck.

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Biological Activity

Description Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.
Targets
Cdc2/CyclinB [1]
()
CDK2/CyclinE [1] CDK2/CyclinA [1] CDK4/CyclinD1 [1]
4 nM 35 nM 70 nM 850 nM
In vitro

Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells.[2] Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells. [3]

Protocol

Cell Research:[2]
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  • Cell lines: MCF-7 and MDA-MB 231 breast cancer cells
  • Concentrations: 100 μM
  • Incubation Time: 24 h
  • Method: 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)

Solubility (25°C)

In vitro DMSO 60 mg/mL warmed (154.28 mM)
Ethanol 13 mg/mL warmed (33.42 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.89
Formula

C19H25ClN6O

CAS No. 212844-53-6
Storage powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID