Cyclophilin inhibitor 1 is an effective and orally bioavailable cyclophilin A inhibitor with a Kd of 5 nM, showing potent anti-HCV activity, and an EC50 for HCV 2a of 98 nM.
Cyclosporin D is a metabolite of cyclosporin A, an immunosuppressant drug that binds cyclophilin D, inhibiting the phosphatase activity of calcineurin in T cells.
RAS RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS RAS-RAF-IN-1 has antitumor activity[1]. RAS RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.