422000

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).

• Synonim(y): 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704
• Wzór empiryczny (zapis Hilla): C₁₆H₁₁BrN₂O
• Numer CAS: 142273-20-9
• Masa cząsteczkowa: 327.18
• Numer MDL: MFCD02683595
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow-brown
• rozpuszczalność: DMSO: 100 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• ciąg SMILES: Brc1cc2c([nH]c3c2CC(=O)Nc4c3cccc4)cc1
• 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)
• Klucz InChI: QQUXFYAWXPMDOE-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3