INY-03-041

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

INY-03-041 

INY-03-041 是一种有效且高度选择性的基于 PROTAC 的泛-AKT 降解物，由与来那度胺 (Cereblon 配体) 偶联的 ATP 竞争性 AKT 抑制剂 GDC-0068 组成。 INY-03-041 抑制 AKT1，AKT2 和 AKT3，IC50 分别为 2.0 nM，6.8 nM 和 3.5 nM。

INY-03-041

INY-03-041 Chemical Structure

CAS No. : 2503017-97-6

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生物活性

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively[1].

IC50 & Target[1]

Akt1

2.0 nM (IC50)

Akt2

6.8 nM (IC50)

Akt3

3.5 nM (IC50)

Cereblon

 

体外研究
(In Vitro)

INY-03-041 (10-1000 nM; 2-24 hours; MDA-MB-468 cells) treatment induces potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared with GDC-0068 in MDA-MB-468 and HCC1937 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 10 nM, 50 nM, 100 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 2 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours
Result: Induced potent degradation of all three AKT isoforms in MDA-MB-468 cells.

分子量

798.41

Formula

C44H56ClN7O5
CAS 号

2503017-97-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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