Name: SHP2 protein degrader-3
Brand: TargetMol
SKU: T211874
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述

SHP2protein degrader-3 is an AUTAC protein degrader specifically targeting SHP2. It induces dose-dependent degradation of SHP2 in HeLa cells, with a DC50 of 3.22 μM, and demonstrates significant antitumor activity with an IC50 of 5.59 μM. The degradation mechanism is mediated via LC3-dependent autophagy, which can be inhibited by lysosomal inhibitors. SHP2protein degrader-3 also induces apoptosis in various tumor cell lines, including cervical cancer cells (HeLa), liver cancer cells (HepG2 and Huh-7), and colon cancer cells (LoVo). [SHP2ligand: ; LC3 Ligand: ; Linker: .]

体外活性

SHP2 protein degrader-3 (Compound SA-8) 在 HeLa 细胞中表现出抗增殖作用，其 IC 50 值分别为24小时5.59 μM、48小时4.25 μM和72小时4.81 μM。SHP2 protein degrader-3 (0-10 μM, 24-96 h) 以时间和剂量依赖性方式降解 HeLa 细胞中的 SHP2 蛋白，具有 3.22 μM 的 DC 50 值，最大降解效率 (D max ) 达到 80.47%。SHP2 protein degrader-3 (10 μM, 72 h) 通过自噬-溶酶体途径诱导 SHP2 蛋白的降解。此外，SHP2 protein degrader-3 (1.1-30 μM, 72 h) 还能在多种癌细胞中，包括 HeLa、HepG2、LoVo 和 Huh-7 细胞，诱导凋亡。