Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13714L |
GRK2-IN-1 hydrochloride (2055990-90-2 free base)
GRK2-IN-1 hydrochloride |
GRK | GPCR/G Protein |
GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM). | |||
T13714 |
CCG258208
GRK2-IN-1 |
GRK | GPCR/G Protein |
GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM). | |||
T79913 |
GRK2 Inhibitor 2
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GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂,对GRK2有显著的抑制活性(IC50: 19 nM),同样对Aurora-A也表现出抑制作用(IC50: 137 nM)。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外,GRK2 Inhibitor 2适用于充血性心力衰竭(HF)的相关研究。 | |||
T35875 | CCG258208 hydrochloride | ||
GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):305... |