Select your Country or Region

  • TargetMol | Compound LibraryArgentinaArgentina
  • TargetMol | Compound LibraryAustraliaAustralia
  • TargetMol | Compound LibraryAustriaAustria
  • TargetMol | Compound LibraryBelgiumBelgium
  • TargetMol | Compound LibraryBrazilBrazil
  • TargetMol | Compound LibraryBulgariaBulgaria
  • TargetMol | Compound LibraryCroatiaCroatia
  • TargetMol | Compound LibraryCyprusCyprus
  • TargetMol | Compound LibraryCzechCzech
  • TargetMol | Compound LibraryDenmarkDenmark
  • TargetMol | Compound LibraryEgyptEgypt
  • TargetMol | Compound LibraryEstoniaEstonia
  • TargetMol | Compound LibraryFinlandFinland
  • TargetMol | Compound LibraryFranceFrance
  • TargetMol | Compound LibraryGermanyGermany
  • TargetMol | Compound LibraryGreeceGreece
  • TargetMol | Compound LibraryHong KongHong Kong
  • TargetMol | Compound LibraryHungaryHungary
  • TargetMol | Compound LibraryIcelandIceland
  • TargetMol | Compound LibraryIndiaIndia
  • TargetMol | Compound LibraryIrelandIreland
  • TargetMol | Compound LibraryIsraelIsrael
  • TargetMol | Compound LibraryItalyItaly
  • TargetMol | Compound LibraryJapanJapan
  • TargetMol | Compound LibraryKoreaKorea
  • TargetMol | Compound LibraryLatviaLatvia
  • TargetMol | Compound LibraryLebanonLebanon
  • TargetMol | Compound LibraryMalaysiaMalaysia
  • TargetMol | Compound LibraryMaltaMalta
  • TargetMol | Compound LibraryMoroccoMorocco
  • TargetMol | Compound LibraryNetherlandsNetherlands
  • TargetMol | Compound LibraryNew ZealandNew Zealand
  • TargetMol | Compound LibraryNorwayNorway
  • TargetMol | Compound LibraryPolandPoland
  • TargetMol | Compound LibraryPortugalPortugal
  • TargetMol | Compound LibraryRomaniaRomania
  • TargetMol | Compound LibrarySingaporeSingapore
  • TargetMol | Compound LibrarySlovakiaSlovakia
  • TargetMol | Compound LibrarySloveniaSlovenia
  • TargetMol | Compound LibrarySpainSpain
  • TargetMol | Compound LibrarySwedenSweden
  • TargetMol | Compound LibrarySwitzerlandSwitzerland
  • TargetMol | Compound LibraryTaiwan,ChinaTaiwan,China
  • TargetMol | Compound LibraryThailandThailand
  • TargetMol | Compound LibraryTurkeyTurkey
  • TargetMol | Compound LibraryUnited KingdomUnited Kingdom
  • TargetMol | Compound LibraryUnited StatesUnited States
  • TargetMol | Compound LibraryOther CountriesOther Countries
Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

GSK269962A

GSK269962A
Contact us for more batch information
Select Batch
Purity:99.14%
Resource Download

GSK269962A

Catalog No. T3518Cas No. 850664-21-0
GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
5 mg$82In Stock
10 mg$123In Stock
25 mg$238In Stock
50 mg$396In Stock
100 mg$579In Stock
1 mL x 10 mM (in DMSO)$108In Stock
Bulk & Custom
Add to Cart

Related Compound Libraries of "GSK269962A"

Product Introduction

Bioactivity
Description
GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
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
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).
Kinase Assay
The enzyme activity and kinetics of the purified ROCK1(3-543) are determined using scintillation proximity assay. In this assay, purified ROCK1 is incubated with peptide substrate (Biotin-Ahx-AKRRLSSLRA-CONH2), and 33ATP and the subsequent incorporation of 33P into the peptide is quantified by streptavidin bead capture. For IC50 determination, test compounds are dissolved at 10 mM in 100% DMSO, with subsequent serial dilution in 100% DMSO. Compounds are typically assayed over an 11-point dilution range with a concentration in the assay of 10 μM to 0.2 nM in 3-fold dilutions. For dose-response curves, data are normalized and expressed as percentage inhibition using the formula 100×[(U-C1)/(C2-C1)], where U is the unknown value, C1 is the average of the high signal (0%) control wells, and C2 is the average of the low signal (100%) control wells. Curve fitting is performed The results for each compound are recorded as pIC50 values[1].
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)
AliasGSK269962B, GSK 269962, GSK269962A HCl
Chemical Properties
Molecular Weight570.6
FormulaC29H30N8O5
Cas No.850664-21-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 57.1 mg/mL(100 mM)
Ethanol: 6 mg/mL (9.88 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.7525 mL8.7627 mL17.5254 mL87.6271 mL
5 mM0.3505 mL1.7525 mL3.5051 mL17.5254 mL
DMSO
1mg5mg10mg50mg
10 mM0.1753 mL0.8763 mL1.7525 mL8.7627 mL
20 mM0.0876 mL0.4381 mL0.8763 mL4.3814 mL
50 mM0.0351 mL0.1753 mL0.3505 mL1.7525 mL
100 mM0.0175 mL0.0876 mL0.1753 mL0.8763 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords