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$0.00 - Katelyn M Green, .et al. High-throughput screening yields several small-molecule inhibitors of repeat-associated non-AUG translation, J Biol Chem, 2019, jbc.RA119.009951
Biological Activity
Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC₅₀ = 400 nM), CDK2/cyclin A (IC₅₀ = 680nM) , CDK5 (IC₅₀ = 850nM) and with much less effect other kinases.
Targets
| Target | Value |
|---|---|
| GSK-3β | IC50: 0.23μM |
| CDK1/CyclinB | IC50: 0.4μM |
| CDK2/CyclinA | IC50: 0.68μM |
| CDK5/p35 | IC50: 0.85μM |
| CDK2/CyclinE | IC50: 7.5μM |
| ERK2 | IC50: 9μM |
| c-Src | IC50: 15μM |
| CaseinKinase2 | IC50: 20μM |
| ERK1 | IC50: 20μM |
| In vitro (25°C) | DMSO | 58 mg/mL (177.27 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+50% PEG 300+5% Tween 80+ddH2O | 2.3 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 30.56 mL | 152.81 mL | 305.62 mL |
| 0.5 mM | 6.11 mL | 30.56 mL | 61.12 mL |
| 1 mM | 3.06 mL | 15.28 mL | 30.56 mL |
| 5 mM | 0.61 mL | 3.06 mL | 6.11 mL |
*The above data is based on the productmolecular weight 327.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11220 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 142273-20-9 |
| Formula | C16H11BrN2O |
| M. Wt | 327.2 |
| Solubility | DMSO |
| Purity | >98% |
| SMILES | C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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