LDLRAP1-IN-1 (Compound B19) is a LDLRAP1 inhibitor and antiviral agent, with an IC50 of 4.98 μM for disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 covalently modifies the C119 residue of LDLRAP1 at the LDLRAP1 - LDLR binding interface, thereby disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 exhibits antiviral activity against HCoV-OC43 [1].
In Vitro, LDLRAP1-IN-1 (5 days potently inhibits HCoV-OC43 infection in Vero E6 cells with an EC50 of 1.0 ± 0.1 μM, while exhibiting low cytotoxicity (CC50 = 151 μM)[1]. LDLRAP1-IN-1 (1 h) disrupts the interaction between LDLRAP1 and LDLR, with an IC50 of 4.98 μM, and reduces the binding affinity by 11.1-fold[1].
References:
[1]. Huang Z, et al. Nitro-Diphenyl Ethers as Emerging Cysteine-Targeting Covalent Warheads Enable Identification of Novel Target LDLRAP1 for Anticoronaviral Activity. J Med Chem. 2026;69(5):5986-6003.
In Vitro, LDLRAP1-IN-1 (5 days potently inhibits HCoV-OC43 infection in Vero E6 cells with an EC50 of 1.0 ± 0.1 μM, while exhibiting low cytotoxicity (CC50 = 151 μM)[1]. LDLRAP1-IN-1 (1 h) disrupts the interaction between LDLRAP1 and LDLR, with an IC50 of 4.98 μM, and reduces the binding affinity by 11.1-fold[1].
References:
[1]. Huang Z, et al. Nitro-Diphenyl Ethers as Emerging Cysteine-Targeting Covalent Warheads Enable Identification of Novel Target LDLRAP1 for Anticoronaviral Activity. J Med Chem. 2026;69(5):5986-6003.