GRK

Other GPCR & G Protein Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor GPR CCR

Cat.No.	Product Name	Information	Product Use Citations
S8489	GSK180736A (GSK180736)	GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.	Cell Rep, 2023, 42(7):112812 Cancer Lett, 2022, 529:112-125
S6621	CCG215022	CCG215022 serves as a pan-G protein-coupled receptor kinases (GRKs) inhibitor with IC50 of 3.9 μM, 0.15 μM, 0.38 μM for GRK1, GRK2, GRK5, respectively.	ACS Omega, 2024, 9(37):38477-38489
E2817	GRK5-IN-2	GRK5-IN-2 is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor.

Cat.No.

Product Name

Information

Product Use Citations

Product Validations

S8489

GSK180736A (GSK180736)

GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.

Cell Rep, 2023, 42(7):112812

Cancer Lett, 2022, 529:112-125

S6621

CCG215022

CCG215022 serves as a pan-G protein-coupled receptor kinases (GRKs) inhibitor with IC50 of 3.9 μM, 0.15 μM, 0.38 μM for GRK1, GRK2, GRK5, respectively.

ACS Omega, 2024, 9(37):38477-38489

E2817

GRK5-IN-2

GRK5-IN-2 is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor.