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126871  Alsterpaullone, 2-Cyanoethyl

3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile

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25 May 2012

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126871-1MG  1 mg 
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A cell-permeable and reversible Alsterpaullone (Cat. No. 126870) derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β (IC50 = 230 pM and 800 pM, respectively; [ATP] = 15 µM). Displays ~37-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC50 = 30 nM). Shown to inhibit other kinases in a commercially available testing screen panel (pIC50 = −logIC50[M]; pIC50 = ~ 7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = 1 µM).
Product information
Form Light orange solid
Primary Target Cdkl/Gsk-3β, Cyclin B
Primary Target IC50 230 pM/800 pM
Secondary target Cdk5/p25 (IC50 = 30 nM)
Molar mass 346.3
Protect from Light Yes
Packaged under inert gas Yes
ATP Competitive Yes
Purity ≥90% by HPLC
Solubility DMSO
Chemical formula C19H14N4O3
CAS number 852529-97-0
Store and ship information
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling
Alsterpaullone, 2-Cyanoethyl, molecular structure

© Merck KGaA, Darmstadt, Germany, 2012

All references to Merck refer to Merck KGaA, Darmstadt, Germany.


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