4-Br-Bnlm

4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC₅₀ value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity^[1][2]. IC50 & Target:EC50: 0.96 µM (glucose-regulated protein 94, Grp94)^[1][2] In Vitro:4-Br-Bnlm (0-100 µM; 24 h) inhibits 1477N mutant myocilin in human embryonic kidney (HEK) cells expression^[1].
4-Br-Bnlm (30 µM; 24 h) reduces mutant myocilin levels and toxicity in primary human trabecular meshwork (HTM) cells^[1].
4-Br-Bnlm (3, 10 and 30 µM; 24 h) inhibits myocilin secretion with dose-dependent manner in myocilin cell^[1].
4-Br-Bnlm (30 µM and 100 µM; 24 h) doesn’t induces a heat shock response in the HTM cells^[2]. In Vivo:4-Br-Bnlm (300 µM; eye drops; once daily for 12 weeks) clears the mutant myocilin within trabecular meshwork (TM) cells and decreases intraocular pressure (IOP) in Tg-MYOC^Y437H mice model. 4-Br-Bnlm improves photopic negative response (PhNR) deficits^[2].