GSK180736A

SKU: orb1304130

Description

GSK180736A is a potent and selective GRK2 inhibitor (IC50 = 0.77 µM) with over 100-fold selectivity for GRK2 over other GRK isoforms. It also effectively inhibits ROCK1 (IC50 = 100 nM) and shows weaker activity against PKA. This compound is a valuable research tool for investigating GPCR signaling and Rho-ROCK pathways in cardiovascular and fibrotic disease models.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 817194-38-0
• MW: 365.36
• Purity: 98.98% (May vary between batches)
• Formula: C₁₉H₁₆FN₅O₂
• SMILES: CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1
• Target: ROCK,GRK,PKA
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.47 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (164.22 mM);Ethanol:3 mg/mL (8.21 mM)

Bioactivity

• Target IC50:
  ROCK1:100 nM|GRK2:0.77 μM
• In Vitro:
  GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).
• Cell Research:
  Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ROK, ROCK, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, PKA, Inhibitor, inhibit, GSK180736, GSK-180736, GSK180736A, GSK-180736A, GSK 180736, GRK1, GRK2, GRK5

Compound Identifiers

PubChem CID

11233873