GSK-180736A

SKU: orb1223944

Description

A highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM; displays >400-fold selective for GRK2 over both GRK1 and GRK5, with no inhibition on PKA; also inhibits ROCK with IC50 of 0.1 uM.

Key Properties

• CAS Number: 817194-38-0
• MW: 365.3611
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆FN₅O₂
• SMILES: CC1=C(C(NC(=O)N1)C2=CC=C(C=C2)F)C(=O)NC3=CC4=C(C=C3)NN=C4
• Target: GRK (GPCRK)
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 180736A | GSK180736A

Quick Database Links

Gene Symbol

GRK (GPCRK)