GSK269962A

SKU: orb1304125

Description

GSK269962A hydrochloride is a potent and selective ROCK inhibitor, exhibiting IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It is widely used in cardiovascular and neurological research to investigate Rho kinase signaling pathways in both cellular and animal models.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 850664-21-0
• MW: 570.6
• Purity: 99.71% (May vary between batches)
• Formula: C₂₉H₃₀N₈O₅
• SMILES: CCn1c(nc2cnc(Oc3cccc(NC(=O)c4ccc(OCCN5CCOCC5)cc4)c3)cc12)-c1nonc1N
• Target: ROCK,S6 Kinase
• Solubility: DMSO:57.1 mg/mL (100.07 mM);Ethanol:6 mg/mL (10.52 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.51 mM)

Bioactivity

• Target IC50:
  AKT3:1510 nM|GSK-3α:1260 nM|AKT1:955 nM|RSK1:132 nM|AKT2:1350 nM|MSK1:49 nM|CDK2:3500 nM|ROCK1:1.6 nM|ROCK2:4 nM
• In Vivo:
  Oral administration of GSK269962A produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. The reduction of blood pressure was acute and substantial. The maximal effect on blood pressure was observed approximately 2 h after oral gavages. The reduction of blood pressure was accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism. ROCK inhibition with the use of GSK 269962 in the 10 mg/kg dose, in turn, triggered an increase in VV(voided volume), PVR(post-void residual), VT(volume threshold), VE(voiding efficiency), ICI(intercontraction interval), BC(bladder compliance), and VTNVC(volume threshold to elicit NVC).
• In Vitro:
  GSK269962A completely abolished the actin stress fiber formation induced by angiotensin II in human smooth muscles. Such suppressive effect on actin fiber formation was observed beginning at around 1 μM GSK269962A. GSK269962A induced vasorelaxation in preconstricted rat aorta(tissue baths) with an IC50 of 35 nM. the relaxation induced by GSK269962A is reversible. GSK269962A suppressed IL-6 mRNA transcription and reduced LPS-induced IL-6 and TNF-α protein production in macrophages
• Cell Research:
  Human primary smooth muscle cells were serum-starved(cells were grown on coverslips, and at approximately 50% confluence, they were serum-starved overnight) and stimulated with AngII (100 nM) for 2 h. ROCK inhibitors (3 μM for SB-772077-B or GSK269962A) were added 30 min before AngII stimulation, and cells were fixed and stained with rhodamine phalloidin. Confocal images of actin stain were obtained.(Only for Reference)

Storage & Handling

• Storage: store under nitrogen | 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

GSK269962B, GSK269962, GSK-269962, GSK269962A, GSK-269962A, GSK269962A HCl, GSK 269962, MSK1, pressure, RSK1, S6 Kinase, S6Kinase, ROCK, ROCK1, ROCK2, vasodilatory

Compound Identifiers

PubChem CID

16095342