Grk2 Inhibitor GSK180736A Cas 817194-38-0
Grk2 Inhibitor GSK180736A Cas 817194-38-0
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Chemical Information
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Product name:GSK180736A |
Purity:98% min |
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CAS NO:817194-38-0 |
Solubility:DMSO30 mg/mL (82.11 mM) |
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Molecular Formula:C19H16FN5O2 |
Package:Package according to customer requirements |
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Molecular Weight:365.3684 |
Storage:Store at -20℃ |
Quality control
Remarks
GSK180736A is potent and selective inhibitor of GRK2 with an IC50 of 0.77 M25 and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA with an IC50 of 30 M, but highly potent against ROCK1 (IC50 = 100 nM).
References
[1].Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.
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