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Alsterpaullone

AG-CR1-0036-M001 1 mg INQ
AG-CR1-0036-M005 5 mg INQ
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Additional Information

Product Data
Synonyms 9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
Properties
Formula C16H11N3O3
MW 293.3
CAS 237430-03-4
Purity ≥98% (NMR)
Appearance Yellow to brown powder.
Solubility Soluble in DMSO; insoluble in water or 100% ethanol.
Identity Determined by IR, 1H-NMR and 13C-NMR.
InChi Key OLUKILHGKRVDCT-UHFFFAOYSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage +4°C
Handling Advice Protect from light.
Use/Stability Stable for at least 2 years after receipt when stored at +4°C.
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Product Description

  • Potent CDK1/cyclin B (IC50 = 35 nM) inhibitor [1].
  • Anti-tumor compound [1]
  • Potent inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC50 = 200 nM), CDK5/p25 (IC50 = 40 nM), CDK5/p35 (IC50 = 40 nM) [2, 4].
  • GSK-3β (glycogen synthase kinase-3β) inhibitor [2, 3].
  • Apoptosis inhibitor [6, 7].
  • Apoptosis inducer [5].
  • Angiogenesis inhibitor [8].

Product References

  1. Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity: C. Schultz, et al.; J. Med. Chem. 42, 2909 (1999)
  2. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25: M. Leost, et al.; Eur. J. Biochem. 267, 5983 (2000)
  3. Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor: M. Knockaert, et al.; J. Biol. Chem. 277, 25493 (2002)
  4. The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003)
  5. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential: T. Lahusen, et al.; Mol Carcinog 36, 183 (2003)
  6. Thapsigargin-induced apoptosis was prevented by glycogen synthase kinase-3 inhibitors in PC12 cells: T. Takadera, et al.; Neurosci. Lett. 408, 124
  7. Colchicine-induced apoptosis was prevented by glycogen synthase kinase-3 inhibitors in PC12 cells: T. Takadera, et al.; Cell. Mol. Neurobiol. 30, 863 (2010)
  8. Anti-angiogenic potential of small molecular inhibitors of cyclin dependent kinases in vitro: S. Zahler, et al.; Angiogenesis 13, 239 (2010)
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