Purvalanol A (Synonyms: NG 60) |
カタログ番号GC14707
One-Click Copy Product Info
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プルバラノール A は強力な CDK 阻害剤であり、cdc2-サイクリン B、cdk2-サイクリン A、cdk2-サイクリン E、cdk4-サイクリン D1、および cdk5-p35 をそれぞれ 4、70、35、850、75 nM の IC50 で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 212844-53-6
Sample solution is provided at 25 µL, 10mM.
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Purvalanol A is a potent and selective inhibitor of CDK with IC50 values of 4, 35, 70, 75 and 850 nM for cdc2-cyclin B, cdk2-cyclin E, cdk2-cyclin A, cdk5-p35 and cdk4-cyclin D1, respectively [1].
Cyclin-dependent kinases (CDKs) are a family of protein kinases and play an important role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells.
In MKN45 cells, purvalanol A (30 μM) reduced the expression of antiapoptotic proteins Bcl-2, Bcl-XL and survivin and induced apoptosis. Also, purvalanol A inhibited the phosphorylation of STAT3 by Janus kinase 2 (JAK2) and the expression and phosphorylation of RNA polymerase II, which was involved in transcriptional regulation [2]. In MCF-7 ER(+) cells, purvalanol A induced apoptosis in a caspase-dependent way and increased the levels of spermidine/spermine N1-acetyltransferase (SSAT) and polyamine oxidase (PAO) [3].
In the dentate gyrus (DG) of the rat hippocampus, purvalanol A (40 nmol/3 μl) significantly induced the number of BrdU-positive cells in a time- and concentration-dependent way [4].
References:
[1]. Gray NS, Wodicka L, Thunnissen AM, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science, 1998, 281(5376): 533-538.
[2]. Iizuka D, Ogura A, Kuwabara M, et al. Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II. Anticancer Drugs, 2008, 19(6): 565-572.
[3]. Obakan P, Ar?san ED, ?zfiliz P, et al. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep, 2014, 41(1): 145-154.
[4]. Ma?kowiak M, Kolasiewicz W, Markowicz-Kula K, et al. Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus. Pharmacol Rep, 2005, 57(6): 845-849.
| Cas No. | 212844-53-6 | SDF | |
| 同義語 | NG 60 | ||
| Chemical Name | (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol | ||
| Canonical SMILES | ClC1=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@@H](CO)C(C)C)=N2)=CC=C1 | ||
| Formula | C19H25ClN6O | M.Wt | 388.89 |
| 溶解度 | ≥ 19.45mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL |
| 5 mM | 514.3 μL | 2.5714 mL | 5.1428 mL |
| 10 mM | 257.1 μL | 1.2857 mL | 2.5714 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)