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GSK215

Catalog No. T67843   CAS 2743427-26-9

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4). GSK215 is designed by the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase. GSK215 can induce rapid and prolonged FAK degradation.

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GSK215 Chemical Structure
GSK215, CAS 2743427-26-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 127.00
5 mg In stock $ 317.00
10 mg In stock $ 497.00
25 mg In stock $ 829.00
50 mg In stock $ 1,150.00
100 mg In stock $ 1,550.00
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Purity: 99.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4). GSK215 is designed by the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase. GSK215 can induce rapid and prolonged FAK degradation.
In vitro GSK215 induced degradation is proteasome and ubiquitin dependent. GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells[1]. GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells. GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[1].
In vivo GSK215 (8 mg/kg; i.h.; once) degrades FAK, and exhibits the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].
Molecular Weight 985.13
Formula C50H59F3N10O6S
CAS No. 2743427-26-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225.0 mg/mL (228.4 mM ), sonification is recommended.

TargetMolReferences and Literature

1. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237.

Related compound libraries

This product is contained In the following compound libraries:
Cytoskeletal Signaling Pathway Compound Library Bioactive Compound Library Tyrosine Kinase Inhibitor Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets
Defactinib FAK-IN-10 AMP-945 Roslin 2 bromide Excisanin A Defactinib hydrochloride AZ7550 ALK inhibitor 1

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Keywords

GSK215 2743427-26-9 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK GSK 215 GSK-215 inhibitor inhibit

 

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