2. Autophagy PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. AUTACs SHP2 Apoptosis Autophagy Atg8/LC3
  4. SHP2 protein degrader-3

SHP2 protein degrader-3 是一种靶向 SHP2 的 AUTAC 蛋白降解剂。SHP2 protein degrader-3 在 HeLa 细胞中剂量依赖性降解 SHP2 (DC50 = 3.22 μM)，并且表现出显著的抗肿瘤活性 (IC50=5.59 μM)。SHP2 protein degrader-3 的降解机制是通过 LC3 介导的自噬 (autophagy) 途径实现的，这一过程可被溶酶体抑制剂所阻断。 SHP2 protein degrader-3 能诱导多种肿瘤细胞 (宫颈癌细胞 (HeLa)，肝癌细胞 (HepG2 和 Huh-7)，结肠癌细胞 (LoVo)) 发生凋亡 (apoptosis)。(SHP2 ligand：(HY-100388)；LC3 Ligand：(HY-10542)；Linker：(HY-128834))。

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SHP2 protein degrader-3

SHP2 protein degrader-3 Chemical Structure

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SHP2 protein degrader-3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC50 = 3.22 μM) and anti-tumor activity (IC50 = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834))[1].

体外研究
(In Vitro)

SHP2 protein degrader-3 (Compound SA-8) (24-72 h) 对 HeLa 细胞显示出抗增殖活性，其 IC50 值分别为：24 小时 5.59 μM、48 小时 4.25 μM 和 72 小时 4.81 μM[1]。
SHP2 protein degrader-3 (0-10 μM, 24-96 h) 在 HeLa 细胞中以时间和剂量依赖的方式降解 SHP2 蛋白，其 DC50 值为 3.22 μM，最大降解效率 (Dmax) 达到 80.47%[1]。
SHP2 protein degrader-3 (10 μM, 72 h) 通过自噬-溶酶体途径诱导 SHP2 蛋白降解[1]。
SHP2 protein degrader-3 (1.1-30 μM, 72 h) 在不同浓度下均可诱导多种癌细胞 (包括 HeLa 细胞、HepG2 细胞、LoVo 细胞和 Huh-7 细胞) 发生凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SHP2 protein degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Blocked SHP2 degradation when Pre-treatment with GW5074 (HY-10542) (1 μM) or SHP099 (HY-100388) (1 μM) for 4 h.
Blocked SHP2 degradation when Pre-treatment with Chloroquine (HY-17589A) (1 μM) or 3-Methyladenine (3-MA) (HY-19312) (0.125 nM/1 μM) for 4 h.
Blocked SHP2 degradation when Pre-treatment with MG132 (HY-13259) (50 nM) for 4 h.
Enhanced SHP2 degradation when Pre-treatment with Rapamycin (HY-10219) (6 μM) for 4 h.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0.12, 0.37, 1.1, 3.3, 10 μM
Incubation Time: 48 h
Result: Increased the LC3 levels in HeLa cells.

Apoptosis Analysis[1]

Cell Line: HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells
Concentration: 1.1, 3.3, 10, 20, 30 μM
Incubation Time: 72 h
Result: Induced apoptosis at different concentrations in HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells.
分子量

1213.58

Formula

C46H51Br2Cl2IN10O7
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.
纯度 & 产品资料
参考文献

SHP2 protein degrader-3 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

SHP2 protein degrader-3AUTACsSHP2ApoptosisAutophagyAtg8/LC3Autophagy-targeting chimerasSrc homology phosphatase 2PTPN11Autophagy-related 8| SHP2HeLa cellsHepG2 cellsLoVo cellsHuh-7 cellsapoptosisautophagyInhibitorinhibitorinhibit

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