© 2008 Alexis Corporation
ALX-270-275
Revised 07-Dec-07
Alsterpaullone
SYNONYMS
9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5
H
)-one
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-275-M001
1 mg
60.00 USD
ALX-270-275-M005
5 mg
270.00 USD
Product Specification
FORMULA:
C
16
H
11
N
3
O
3
MW:
293.3
CAS NUMBER:
237430-03-4
PURITY:
≥95% (HPLC)
APPEARANCE:
Yellow to brown powder.
SOLUBILITY:
Soluble in DMSO; insoluble in water or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
IDENTITY:
Identity determined by IR,
1
H-NMR and
13
C-NMR.
Product Description
Potent inhibitor of CDK1/cyclin B (IC
50
=35nM). Potent and selective inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC
50
=200nM), CDK5/p25 (IC
50
=40nM), CDK5/p35 (IC
50
=40nM) and GSK-3β . Induces apoptosis by activation of caspase-8 and caspase-9 followed by disruption of the mitochondrial potential.
Licensed from NCI.
Product Specific Literature References
ATP-site directed inhibitors of cyclin-dependent kinases
:
N. Gray, et al.; Curr. Med. Chem.
6
, 859 (1999)
Abstract
Fused azepinones with antitumor activity:
C. Kunick; Curr. Pharm. Des.
5
, 181 (1999), (Review)
Abstract
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)
Abstract
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases
:
D.W. Zaharevitz, et al.; Cancer Res.
59
, 2566 (1999)
Abstract
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity
:
C. Kunick, et al.; Bioorg. Med. Chem. Lett.
10
, 567 (2000)
Abstract
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)
Abstract
Inhibition of CDKs as a therapeutic modality
:
E.A. Sausville, et al.; Ann. NY Acad. Sci.
910
, 207 (2000)
Abstract
A novel, extraneuronal role for cyclin-dependent protein kinase 5 (CDK5): modulation of cAMP-induced apoptosis in rat leukemia cells
:
T. Sandal, et al.; J. Biol. Chem.
277
, 20783 (2002)
Abstract
;
Full Text
Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor
:
M. Knockaert, et al.; J. Biol. Chem.
277
, 25493 (2002)
Abstract
;
Full Text
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)
Abstract
The specificities of protein kinase inhibitors: an update
:
J. Bain, et al.; Biochem. J.
371
, 199 (2003)
Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
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