GNE-064 是一种选择性的，具有口服活性的以及高可溶性的 SMARCA4，SMARCA2 和 PBRM1 bromodomains 5 抑制剂。GNE-064 对 SMARCA4 具有抑制作用，其 IC50 值为 0.035 μM，对 SMARCA2 也具有抑制作用，其 EC50 值为 0.10 μM。GNE-064 对 SMARCA4，SMARCA2，PBRM1 bromodomains 5 和 PBRM1 bromodomains 2 的 Kd 值为 0.01，0.016，0.018 以及 0.049 μM。GNE-064 可以作为一种药物探针，用于药物合成的研究。

GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.

GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1].

GNE-064 (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice [1].

1997321-20-6

C17H21N5O2

327.38

GNE064

DMSO:112.5mg/mL (343.6mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years