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Key Documents

Altri documenti

422000

Sigma-Aldrich

Kenpaullone

A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks).

Sinonimo/i:

Kenpaullone, 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704

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About This Item

Formula empirica (notazione di Hill):
C16H11BrN2O
Numero CAS:
142273-20-9
Peso molecolare:
327.18
Numero MDL:
MFCD02683595
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥95% (HPLC)

Forma fisica

solid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze
protect from light

Colore

yellow-brown

Solubilità

DMSO: 100 mg/mL

Condizioni di spedizione

ambient

Temperatura di conservazione

−20°C

InChI

1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
QQUXFYAWXPMDOE-UHFFFAOYSA-N

Descrizione generale

A potent cell-permeable and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding.
A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding.

Azioni biochim/fisiol

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 230 nM, 470 nM, 400 nM, 680 nM, 7.5 µM, 850 nM, 15 µM, 20 µM, 20 µM, 9 µM against glycogen synthase kinase-3β, Lck IC50, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, c-Src, casein kinase II, ERK1, and ERK2

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

Bain, J., et al. 2003. Biochem. J. 371, 199.
Buolamwini, J.K. 2000. Curr. Pharm. Des.6, 379.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Certificati d'analisi (COA)

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