GSK180736A


CAS No. : 817194-38-0

817194-38-0
Price and Availability of CAS No. : 817194-38-0
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2mg $60 In-stock
5mg $90 In-stock
10mg $120 In-stock
25mg $235 In-stock
50mg $400 In-stock
100mg $750 In-stock
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Cat. No. : HY-18990
M.Wt: 365.36
Formula: C19H16FN5O2
Purity: >98 %
Solubility: DMSO : ≥ 30 mg/mL
Introduction of 817194-38-0 :

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. IC50 & Target: IC50: 0.77 μM (GRK2), 100 nM (ROCK1)[1] In Vitro: GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM)[1].

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