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GRK5-IN-5 (Compound 4a) is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5) with an IC50 value of 0.03 μM. It shows an IC50 of 2.2 μM for GRK2 and 0.036 μM for GRK6. GRK5-IN-5 exhibits potent anti-hypertrophic activity in cardiac muscle and inhibits the proliferation of non-cardiac cells. It blocks pathological cardiac remodeling by inhibiting the abnormal upregulation of hypertrophic marker genes Nppa and Nppb. GRK5-IN-5 is useful for research in myocardial hypertrophy.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | GRK5-IN-5 (Compound 4a) is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5) with an IC50 value of 0.03 μM. It shows an IC50 of 2.2 μM for GRK2 and 0.036 μM for GRK6. GRK5-IN-5 exhibits potent anti-hypertrophic activity in cardiac muscle and inhibits the proliferation of non-cardiac cells. It blocks pathological cardiac remodeling by inhibiting the abnormal upregulation of hypertrophic marker genes Nppa and Nppb. GRK5-IN-5 is useful for research in myocardial hypertrophy. |
| Targets&IC50 | GRK5:0.03 μM |
| Molecular Weight | 542.57 |
| Formula | C30H27FN4O5 |
| Cas No. | 3061801-11-1 |
| Smiles | C(=C\1/C=2C(NC1=O)=CC=C(C(N[C@H](C)C3=CC=C(F)C=C3)=O)C2)\C4=C(C)C(NC([C@@H](O)C5=CC=CO5)=O)=C(C)N4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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