cyclophilin inhibitor 1

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.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.

RAS RAS-RAF-IN-1 is a potent inhibitor of RAS and RAS-RAF, exhibiting a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity and demonstrating antitumor activity[1].

CRV431 is a novel Pan-Cyclophilin Inhibitor, potently inhibiting all cyclophilin isoforms tested - A, B, D, and G (IC50 values ranged from 1-7 nM).

CypD-IN-3, a potent and subtype-selective cyclophilin D (CypD) inhibitor, exhibits a high affinity for CypD with an IC50 value of 0.01 μM. It is applicable in the research of various conditions, such as oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes [1].

CypD-IN-4 is a potent, subtype-selective cyclophilin D (CypD) inhibitor exhibiting a high affinity for CypD with an IC50 value of 0.057 μM. This compound is utilized in the research of various diseases, such as oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes [1].

CypD-IN-1, a potent and subtype-selective inhibitor targeting cyclophilin E (CypE), demonstrates high affinity with IC50 and Ki values of 0.013 μM and 0.072 μM, respectively. This compound is valuable for research into various conditions, including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes [1].