3061801-11-1
Chemical Structure
GRK5-IN-5
- CAS No.: 3061801-11-1
- Formula:C30H27FN4O5
- Molecular Weight:542.56
InChIKey: XSBCFLGDNDHVIP-ZQAWARHGSA-N
SMILES: O=C(C1=CC2=C(NC(/C2=C\C3=C(C)C(NC([C@@H](O)C4=CC=CO4)=O)=C(C)N3)=O)C=C1)N[C@H](C)C5=CC=C(F)C=C5
Biological Activity: GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy[1].
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GRK5-IN-5 | GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy. | |||||||||||||||||||||
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