126871 Sigma-AldrichAlsterpaullone, 2-Cyanoethyl - CAS 852529-97-0 - Calbiochem
A cell-permeable and reversible Alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β.
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Synonyms: 3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile
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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 852529-97-0 | C₁₉H₁₄N₄O₃ |
| Description | |
|---|---|
| Overview | 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). |
| Catalogue Number | 126871 |
| Brand Family | Calbiochem® |
| Synonyms | 3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile |
| References | |
|---|---|
| References | Kunick, C., et al. 2005. ChemBioChem. 6, 541. |
| Product Information | |
|---|---|
| CAS number | 852529-97-0 |
| ATP Competitive | Y |
| Form | Light orange solid |
| Hill Formula | C₁₉H₁₄N₄O₃ |
| Chemical formula | C₁₉H₁₄N₄O₃ |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | Cdkl/Gsk-3β, Cyclin B |
| Primary Target IC<sub>50</sub> | 230 pM and 800 pM, [ATP] = 15 µM, against Cdk1/cyclin B and GSK-3β, respectively |
| Purity | ≥90% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 126871 | 0 |