CMPD101 Inhibitor

CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18nM and 5.4nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCalpha (IC50s: 3.1uM, 2.3uM, 1.4uM and 8.1uM).

Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential treatment,of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.
Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential treatment,of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.
Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.
Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.

Small volumes of CMPD101, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5754729 is an inhibitor targeting CMPD101.