SHP2-IN-8

发表于由

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。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
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]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务