Catalog No.: PC-49210Not For Human Use, Lab Use Only.
GNE-064 (GNE064) is a potent, selective, and orally bioavailable inhibitor of the bromodomains of SMARCA2 (BRM), SMARCA4 (BRG1) and PBRM1 (polybromo-1) bromodomain 5 (PBRM1(5)) with IC50 of 10 nM, 16 nM and 18 nM, respectively.
GNE-064 (GNE064) is a potent, selective, and orally bioavailable inhibitor of the bromodomains of SMARCA2 (BRM), SMARCA4 (BRG1) and PBRM1 (polybromo-1) bromodomain 5 (PBRM1(5)) with IC50 of 10 nM, 16 nM and 18 nM, respectively.
GNE-064 exhibits modest affinity for PBRM1(2) (IC50, 490 nM), and low micromolar affinity for BRD7 and BRD9, >250-fold selective for SMARCA2, SMARCA4, and PBRM1(5) compared to all nonfamily VIII bromodomains.
GNE-064 showed sub-μM activity (IC50=0.1 uM) in an engineered cellular target-engagement assay, had highly soluble, and demonstrated promising stability in hepatocytes.
