1. Cell Cycle/DNA Damage
    Autophagy
    Apoptosis
  2. CDK
    Autophagy
    Apoptosis
  3. Purvalanol A

Purvalanol A (Synonyms: NG-60)

Cat. No.: HY-18299A Purity: 99.11%
Handling Instructions

Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.

For research use only. We do not sell to patients.

Purvalanol A Chemical Structure

Purvalanol A Chemical Structure

CAS No. : 212844-53-6

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10 mM * 1  mL in DMSO USD 55 In-stock
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100 mg USD 250 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.

IC50 & Target[1]

cdc2-cyclin B

4 nM (IC50)

cdk2-cyclin E

35 nM (IC50)

cdk2-cyclin A

70 nM (IC50)

cdk4-cyclin D1

850 nM (IC50)

cdk5-p35

75 nM (IC50)

erk1

9000 nM (IC50)

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[1]. 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[2]. 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[3].

Molecular Weight

388.89

Formula

C₁₉H₂₅ClN₆O

CAS No.

212844-53-6

SMILES

CC([[email protected]@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (128.57 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5714 mL 12.8571 mL 25.7142 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL
10 mM 0.2571 mL 1.2857 mL 2.5714 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Purvalanol ANG-60NG60NG 60CDKAutophagyApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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Purvalanol A
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HY-18299A
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