CMPD101 是膜透性的GRK2/3高选择性小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM，可研究心衰疾病。

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, significantly reduces the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line[1]. CMPD101 (3-30 μM; pre-30 minutes) does not influence the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30?μM. This compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375. Which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101and it also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues[2].

865608-11-3

C24H21F3N6O

466.46

DMSO:250 mg/mL (535.95 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years