For research use only. Not for therapeutic Use.
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].
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].
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-MYOCY437H mice model. 4-Br-Bnlm improves photopic negative response (PhNR) deficits[2].
| Catalog Number | I042032 |
| CAS Number | 1654775-71-9 |
| Synonyms | methyl 2-[2-[1-[(4-bromophenyl)methyl]imidazol-2-yl]ethyl]-3-chloro-4,6-dihydroxybenzoate |
| Molecular Formula | C20H18BrClN2O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H18BrClN2O4/c1-28-20(27)18-14(19(22)16(26)10-15(18)25)6-7-17-23-8-9-24(17)11-12-2-4-13(21)5-3-12/h2-5,8-10,25-26H,6-7,11H2,1H3 |
| InChIKey | FHDUIAYTJZAXNW-UHFFFAOYSA-N |
| SMILES | COC(=O)C1=C(C(=C(C=C1O)O)Cl)CCC2=NC=CN2CC3=CC=C(C=C3)Br |
| Reference | [1]. Stothert AR, et al, Fontaine SN, Crowley VM, Mishra S, Blagg BS, Lieberman RL, Dickey CA. Exploiting the interaction between Grp94 and aggregated myocilin to treat glaucoma. Hum Mol Genet. 2014 Dec 15;23(24):6470-80. [2]. Stothert AR, et al. Isoform-selective Hsp90 inhibition rescues model of hereditary open-angle glaucoma. Sci Rep. 2017 Dec 20;7(1):17951. |
