Name: SHP2 protein degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

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IUPACName

4-[2-[2-[2-[2-[2-[4-[[[1-[6-amino-5-(2,3-dichlorophenyl)pyrazin-2-yl]-4-methylpiperidin-4-yl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione

Synonyms

1H-Isoindole-1,3(2H)-dione, 4-[[14-[4-[[[1-[6-amino-5-(2,3-dichlorophenyl)-2-pyrazinyl]-4-methyl-4-piperidinyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-3,6,9,12-tetraoxatetradec-1-yl]amino]-2-(2,6-dioxo-3-piperidinyl)-; 4-[[14-[4-[[[1-[6-Amino-5-(2,3-dichlorophenyl)-2-pyrazinyl]-4-methyl-4-piperidinyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-3,6,9,12-tetraoxatetradec-1-yl]amino]-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione; 4-((14-(4-(((1-(6-Amino-5-(2,3-dichlorophenyl)pyrazin-2-yl)-4-methylpiperidin-4-yl)amino)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12-tetraoxatetradecyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

Density

1.49±0.1 g/cm3

InChI Key

PVZCLGQITBYVPH-UHFFFAOYSA-N

InChI

InChI=1S/C42H51Cl2N11O8/c1-42(10-13-53(14-11-42)33-25-47-37(38(45)49-33)29-5-2-6-30(43)36(29)44)48-24-27-26-54(52-51-27)15-17-61-19-21-63-23-22-62-20-18-60-16-12-46-31-7-3-4-28-35(31)41(59)55(40(28)58)32-8-9-34(56)50-39(32)57/h2-7,25-26,32,46,48H,8-24H2,1H3,(H2,45,49)(H,50,56,57)

SMILES

CC1(CCN(CC1)C2=CN=C(C(=N2)N)C3=C(C(=CC=C3)Cl)Cl)NCC4=CN(N=N4)CCOCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O

Mechanism

Target: Targets SHP2 protein tyrosine phosphatase for experimental targeted protein degradation studies.

Binding Site: Binds the SHP2 allosteric phosphatase pocket and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: SHP2 protein degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward SHP2 protein tyrosine phosphatase. The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• PROTAC-Mediated SHP2 Degradation: This product facilitates the targeted degradation of SHP2, a critical phosphatase involved in multiple signaling pathways. Researchers can utilize SHP2 protein degrader-1 to study the downstream effects of SHP2 loss, enhancing understanding of its role in cellular signaling and disease pathogenesis.

• Cancer Research Applications: SHP2 protein degrader-1 is instrumental in cancer research, allowing scientists to investigate the impact of SHP2 degradation on tumor growth and survival. This application aids in elucidating potential therapeutic strategies targeting SHP2 in oncogenic signaling pathways.

• Signal Transduction Studies: By employing SHP2 protein degrader-1, researchers can dissect the intricacies of signal transduction networks. The targeted degradation of SHP2 offers insights into its regulatory functions and interactions within these pathways, advancing the study of cellular communication and response mechanisms.

• Drug Resistance Mechanism Exploration: Utilize SHP2 protein degrader-1 to explore mechanisms of drug resistance linked to SHP2. This application supports the investigation of how SHP2 degradation affects resistance pathways, providing valuable data for developing more effective therapeutic interventions.

1. Novel PROTACs for degradation of SHP2 protein.

Zheng, M., Liu, Y., Wu, C., Yang, K., Wang, Q., Zhou, Y., Chen, L. and Li, H., 2021. Bioorganic Chemistry, 110, p.104788.

Protein tyrosine phosphatase SHP2 is a member of PTPs family associated with cancer such as leukemia, non-small cell lung cancer, breast cancer, and so on. SHP2 is a promising target for drug development, and consequently it is of great significance to develop SHP2 inhibitors. Herein, we report CRBN-recruiting PROTAC molecules targeting SHP2 by connecting pomalidomide with SHP099, an allosteric inhibitor of SHP2. Among them, SP4 significantly inhibited the growth of Hela cells, compared with SHP099, its activity increased 100 times. In addition, it can significantly induce SHP2 degradation and cell apoptosis. Further study of SHP2-protac may have important significance for the treatment of SHP2 related diseases.

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It is commonly abbreviated as: C₁V₁ = C₂V₂