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Key Documents

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).

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C16H11BrN2O
Numéro CAS:
142273-20-9
Poids moléculaire :
327.18
Numéro MDL:
MFCD02683595
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥95% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

yellow-brown

Solubilité

DMSO: 100 mg/mL

Conditions d'expédition

ambient

Température de stockage

−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)

Clé InChI

QQUXFYAWXPMDOE-UHFFFAOYSA-N

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

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Consulter la Bibliothèque de documents

Bryan A Johnson et al.
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While SARS-CoV-2 continues to adapt for human infection and transmission, genetic variation outside of the spike gene remains largely unexplored. This study investigates a highly variable region at residues 203-205 in the SARS-CoV-2 nucleocapsid protein. Recreating a mutation found in
Jonathan Bayerl et al.
Cell stem cell, 28(9), 1549-1565 (2021-04-30)
Isolating human MEK/ERK signaling-independent pluripotent stem cells (PSCs) with naive pluripotency characteristics while maintaining differentiation competence and (epi)genetic integrity remains challenging. Here, we engineer reporter systems that allow the screening for defined conditions that induce molecular and functional features of

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