Nec-4

Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC₅₀ of 2.6 μM, K_i of 0.46 μM. IC50 & Target: IC50: 2.6 μM (RIP1)^[1]. In Vitro: Nec-4 (compound 9) is a slightly better competitor than 7 with a lower K_i value that is similar to R-3. Nec-4 is again a slightly better competitor than Rac-3 with K_i and IC₅₀ values comparable to 7 (Nec-4: IC₅₀=2.6±0.1 μM, K_i=0.46±0.05 μM; 7: IC₅₀=10.7±1.8 μM, K_i=4.5±0.9 μM). Overall, all three compounds cross-compete with each other but Nec-4 is able to more effectively displace both 20 and 26 in comparison to the parent compounds Rac-3 and 7, respectively. This suggests that Nec-4 binding likely significantly overlaps with both the Nec-1 and the Nec-3 binding sites.