grk5 in 2

GRK5-IN-2 是基于吡啶的双环化合物，抑制 G 蛋白偶联受体激酶 5 。它调节胰岛素的表达和 或释放，在代谢疾病中有研究价值。

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).

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).

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):3052-3069.

(S)-Ro 32-0432是一种高效、选择性的ATP竞争性PKC抑制剂，具备口服活性，对PKCα、PKCβI、PKCβII、PKCγ和PKCε的IC50值分别为9.3 nM、28 nM、30 nM、36.5 nM和108.3 nM。此外，(S)-Ro 32-0432也能选择性地抑制GRK5。它能够防止T细胞活化，适用于慢性炎症和自身免疫性疾病的研究。