Alsterpaullone, cyclin-dependent kinase (CDK) and GSK-3beta inhibitor (ab141070)
- Datasheet
- References
Overview
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Product name
Alsterpaullone, cyclin-dependent kinase (CDK) and GSK-3beta inhibitor -
Description
Potent cyclin-dependent kinase (CDK) and GSK-3β inhibitor -
Biological description
Potent CDK inhibitor (IC50 values are 3.5 (CDK1/cyclin B), 20 (CDK2/cyclin A) and 40 nM (CDK5/p35)). Also displays potent and selective inhibition of GSK-3β (IC50 values are 40 and 4 nM respectively). Antiproliferative effects seen in vitro. Cell-permeable. -
Purity
> 96% -
CAS Number
237430-03-4 -
Chemical structure
Properties
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Chemical name
7,12-Dihydro-9-nitroindolo[3,2-d][1]benzazepin-6(5H)-one -
Molecular weight
293.28 -
Molecular formula
C16H11N3O3 -
PubChem identifier
5005498 -
Storage instructions
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
[O-][N+](=O)c4cc3c(NC1C3CC(=O)Nc2ccccc12)cc4 -
Source
Synthetic
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Research areas
- Biochemicals
- Research Area
- Alzheimer's Disease
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
- Biochemicals
- Research Area
- Alzheimer's Disease
- Signaling
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
- Biochemicals
- Research Area
- Diabetes
- Signaling
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
- Biochemicals
- Research Area
- Hypertension
- Signaling
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
- Biochemicals
- Research Area
- Obesity
- Signaling
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
- Biochemicals
- Research Area
- Pain & inflammation
- Apoptosis & cell cycle
- Cyclin-dependent kinase
- Inhibitors
Images
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Functional Studies - Alsterpaullone, cyclin-dependent kinase (CDK) and GSK-3beta inhibitor (ab141070)ab32505 staining AKT1 in SK-N-SH cells treated with alsterpaullone (ab141070), by ICC/IF. Decrease of AKT1 expression correlates with increased concentration of alsterpaullone, as described in literature.
The cells were incubated at 37°C for 6h in media containing different concentrations of ab141070 (alsterpaullone) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab32505 (1/200 dilution was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
References
This product has been referenced in:
- Zahler S et al. Anti-angiogenic potential of small molecular inhibitors of cyclin dependent kinases in vitro. Angiogenesis 13:239-49 (2010). Read more (PubMed: 20706783) »
- Lahusen T et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog 36:183-94 (2003). Read more (PubMed: 12669310) »
- Sandal T et al. A novel, extraneuronal role for cyclin-dependent protein kinase 5 (CDK5): modulation of cAMP-induced apoptosis in rat leukemia cells. J Biol Chem 277:20783-93 (2002). Read more (PubMed: 11909854) »
- Schultz C et al. Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J Med Chem 42:2909-19 (1999). Read more (PubMed: 10425100) »
