ipatasertib

Ipatasertib (GDC-0068) 是选择性的，ATP 竞争性的pan-Akt 抑制剂，能够抑制Akt1 (IC50:5 nM)，Akt2 (IC50:18 nM)，Akt3 (IC50:8 nM)。Ipatasertib (GDC-0068)可以通过抑制Akt导致p53非依赖性PUMA激活，从而同步激活FoxO3a和NF-κB，直接与 PUMA启动子结合，上调 PUMA 转录和 Bax 介导的内在线粒体凋亡。

BMS-986034 is a GPR119 agonist.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for the target protein AKT used in PROTAC, binding to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 for AKT degradation[1].

Ipatasertib-NH2 dihydrochloride is a ligand for the target protein AKT in PROTAC INY-03-041. INY-03-041 consists of Ipatasertib-NH2, a ten-hydrocarbon linker, and the CRBN ligand Lenalidomide, which acts as an E3 ubiquitin ligase.

INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于PROTAC 的泛-AKT 降解剂，由ATP 竞争性AKT 抑制剂Ipatasertib 结合Lenalidomide 组成。INY-03-041 trihydrochloride 可抑制AKT1，AKT2和AKT3，IC50分别为 2.0 nM，6.8 nM 和 3.5 nM。