GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively.
Cat.No
DC10936
Name
GSK3179106
Chemical Properties
CAS
1627856-64-7
Formula
C22H21F4N3O4
MW
467.421
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
Human RET kinase cytoplasmic domain is expressed as an N-terminal GST-fusion protein using a baculovirus expression system. GST-RET is purified using glutathione sepharose chromatography. The RET kinase enzymatic assay is performed in a total volume of 10 uL with increasing concentrations of RET kinase inhibitor as a singlet in a 384 well format as follows: RET inhibitor compound plates are prepared by adding 100 nL of RET inhibitor at different concentrations to a 384-well plate. 5 μE/well of a 2X enzyme mix (50 mM HEPES; 1 mM CHAPS; 0.1 mg/mL BSA; 1 mM DTT; 0.2 nM RET kinase) is added to the 384-well plate and incubated for 30 minutes at 23°C. 5 μE/well of a 2X substrate mix (50 mM HEPES; 1 mM CHAPS; 0.1 mg/mL BSA; 20 μM adenosine triphosphate; 20 mM MgCl2 and 1 μM biotinylated peptide substrate) is added and incubated for 1 hour at 23°C. 10 μE/well of 2X stop/detection mix (50 mM HEPES; 0.1 % BSA; 800 mM Potassium Fluoride; 50 mM EDTA; 200 X dilution of Europium Cryptate labeled anti- phosphotyrosine antibody; 62.5 nM Streptavidin-XL665) incubated for 1 hour at 23°C and read on a Homogenous Time-Resolved Fluorescence reader. IC50s are fitted using GraphPad Prism to a sigmoidal dose response[1].
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