SHP2 protein degrader-1

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SHP2 protein degrader-1 

SHP2 protein degrader-1 是一种有效的 SHP2 变构抑制剂。SHP2 蛋白降解剂-1 诱导 SHP2 降解和细胞凋亡。SHP2 蛋白降解剂-1 具有研究 SHP2 相关疾病的潜力。

SHP2 protein degrader-1

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

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生物活性

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]

体外研究
(In Vitro)

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

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

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

Formula

C42H51Cl2N11O8

CAS 号

2624181-69-5

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]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788.

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