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Alsterpaullone (CAS 237430-03-4)

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Synonym:9-Nitropaullone
Application:A potent ATP-competitive and cell cycle cylin-dependent kinase inhibitor
CAS Number:237430-03-4
Purity:>95%
Molecular Weight:293.28
Molecular Formula:C16H11N3O3
Refer to Certificate of Analysis for lot specific data (including water content).
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Product NameCatalog #UnitPriceQtyAddFavorites
Alsterpaullone sc-202453 1 mg $60
Alsterpaullone sc-202453A 5 mg $294
Description
Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone (sc-208152). The paullones belong to a family of benzazepinones, and are described to highly inhibit neuronal CDK5/p25 and glycogen synthase kinase-3β (GSK-3β). Studies report that Alsterpaullone activates caspase-9 and enhances apoptosis in Jurkat cells, inhibits CDK5/p25-dependent phosphorylation of DARPP-32 in in vitro mouse striatum slices, and blocks the phosphorylation of Tau by GSK-3β.
Technical Information
Appearance:Powder
Physical State:Solid
Solubility:Soluble in DMSO (≥10 mg/ml). Insoluble in water, and 100% ethanol.
Storage:Store at -20° C
Melting Point:238.72 °C (Predicted)
Boiling Point:651.53 °C at 760 mmHg (Predicted)
Density:1.46 g/cm3 (Predicted)
Refractive Index:n20D 1.74 (Predicted)
IC50:CDK1/cyclin B: IC50 = 35 nM; CDK2/cyclin E: IC50 = 200 nM; CDK5/p25: IC50 = 40 nM; CDK5/p35: IC50 = 40 nM; GSK-3β: IC50 = 4 nM; Glycogen synthase kinase-3 alpha: IC50 = 4 nM (human)
Ki Data:CDK2: Ki= 80 nM (human); Glycogen synthase kinase 3: Ki= 0.11 µM (human); LCK: Ki= 0.47 µM (human)
pK Values:pKb: 1.02 (Predicted)
Safety and Reference Information
WGK Germany:3
PubChem CID:5005498
MDL Number:MFCD02683579
SMILES:C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)[N+](=O)[O-]
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1. Leost, M., et al., 2000. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. European journal of biochemistry / FEBS. 267(19): 5983-94. PMID: 10998059
2. Lahusen, Tyler., et al., 2003. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Molecular carcinogenesis. 36(4): 183-94. PMID: 12669310
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