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).

• Szinonimák: Kenpaullone, 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704
• Tapasztalati képlet (Hill-képlet): C₁₆H₁₁BrN₂O
• CAS-szám: 142273-20-9
• Molekulatömeg: 327.18
• MDL-szám: MFCD02683595
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• form: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: yellow-brown
• oldhatóság: DMSO: 100 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: −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)
• Nemzetközi kémiai azonosító kulcs: QQUXFYAWXPMDOE-UHFFFAOYSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3