CRTh2 antagonist 3

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 (compound 4) also enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2].

Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1

Research Areas >> Cardiovascular Disease

Research Areas >> Inflammation/Immunology

CRTh2[1] EC50: 2 μM (PDK1)[2] Ki: 8.4 μM (PDK1)[2]

[1]. Heinz Fretz, et al. 2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists. US8273740.

[2]. Rettenmaier TJ, et al. Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking. J Med Chem. 2015 Oct 22;58(20):8285-8291.