INY-03-041 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 (HY-15186) 结合 Lenalidomide (HY-A0003，Cereblon 配体)组成。INY-03-041 可抑制 AKT1，AKT2 和

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC 50 s of 2.0, 6.8 and 3.5 nM, respectively.

Solid

Akt1 2.0 nM (IC50) Akt3 3.5 nM (IC50

INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells.
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM).
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells.
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7.
[2]. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther. 2012 Feb;11(2):317-28.