126870
Alsterpaullone
A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC50 = 4 nM) and Cdk1/cyclin B (IC50 = 35 nM).
Synonyme(s) :
Alsterpaullone, 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701
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A propos de cet article
Formule empirique (notation de Hill) :
C16H11N3O3
Numéro CAS:
Poids moléculaire :
293.28
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Service technique
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Laissez-nous vous aiderQuality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light yellow to brown
solubility
DMSO: 20 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
[N+](=O)([O-])c1cc2c([nH]c3c2CC(=O)Nc4c3cccc4)cc1
InChI
1S/C16H11N3O3/c20-15-8-12-11-7-9(19(21)22)5-6-14(11)18-16(12)10-3-1-2-4-13(10)17-15/h1-7,18H,8H2,(H,17,20)
InChI key
OLUKILHGKRVDCT-UHFFFAOYSA-N
General description
A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC50 = 35 nM) and GSK-3β (IC50 = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3′,5′-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC50 in the nanomolar range.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
GSK-3β, Cdk1/cyclin B
GSK-3β, Cdk1/cyclin B
Product competes with ATP.
Reversible: yes
Target IC50: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
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Contenu apparenté
Marissa Cloutier et al.
Nature communications, 13(1), 2516-2516 (2022-05-07)
X-chromosome inactivation is a paradigm of epigenetic transcriptional regulation. Female human embryonic stem cells (hESCs) often undergo erosion of X-inactivation upon prolonged culture. Here, we investigate the sources of X-inactivation instability by deriving new primed pluripotent hESC lines. We find