PROTAC SHP2 degrader-1

Modify Date: 2024-01-30 16:01:14

PROTAC SHP2 degrader-1 Structure
PROTAC SHP2 degrader-1 structure
Common Name PROTAC SHP2 degrader-1
CAS Number 2458219-65-1 Molecular Weight 1115.89
Density N/A Boiling Point N/A
Molecular Formula C56H79ClN12O6S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PROTAC SHP2 degrader-1


PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent[1].

 Names

Name PROTAC SHP2 degrader-1

 PROTAC SHP2 degrader-1 Biological Activity

Description PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent[1].
Related Catalog
In Vitro PROTAC SHP2 degrader-1 (0, 3, 10, 30, 100, 300 nM; 12 hours) effectively reduces SHP2 protein in a dosedependent manner, with a DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively[1]. PROTAC SHP2 degrader-1 (100 nM; 0, 2, 4, 8, 12, 24 hours) reduces the SHP2 protein level within 4 h and complete SHP2 depletion with 8 h in KYSE520 and MV-4-11 cells[1]. PROTAC SHP2 degrader-1 (0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells;4 days) achieves IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively[1]. Cell Proliferation Assay[1] Cell Line: KYSE520 and MV-4-11 cells Concentration: 0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells Incubation Time: 4 days Result: Achieved IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively. Western Blot Analysis[1] Cell Line: KYSE520 and MV-4-11 cells Concentration: 0, 3, 10, 30, 100, 300 nM Incubation Time: 12 hours Result: Reduced SHP2 protein in a dosedependent manner, with a DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively. Western Blot Analysis[1] Cell Line: KYSE520 and MV-4-11 cells Concentration: 100 nM Incubation Time: 0, 2, 4, 8, 12, 24 hours Result: Reduced the SHP2 protein level within 4 h and completed SHP2 depletion with 8 h.
References

[1]. Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein [published correction appears in J Med Chem. 2021 Jan 14;64(1):906-908]. J Med Chem. 2020;63(14):7510-7528.

 Chemical & Physical Properties

Molecular Formula C56H79ClN12O6S2
Molecular Weight 1115.89
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.