2707510-30-1

GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM)[1].

HSPA5: 0.59 μM (IC₅₀)

[1] Andrew J Ambrose, et al. Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78. J Med Chem. 2022 Dec 14. DOI:10.1021/acs.jmedchem.2c01631