GSK429286A

Catalog No.S1474 Batch:S147403

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Technical Data

Formula

C21H16F4N4O2
Molecular Weight 432.37 CAS No. 864082-47-3
Solubility (25°C)* In vitro DMSO 86 mg/mL (198.9 mM)
Ethanol 5 mg/mL (11.56 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
15% Captisol citrate vehicle
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol+citrate vehicle clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results. 
Clear solution
2% DMSO 40% PEG300 5%Tween80 53%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
Targets
ROCK1 [1]
(Cell-free assay)		 ROCK2 [2]
(Cell-free assay)
14 nM 63 nM
In vitro GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM. [1] GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho. [2]
In vivo GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg. [1]
Features Greater selectivity than Y-27632.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Male spontaneously hypertensive rats (SHRs)

  • Dosages

    ~30 mg/kg

  • Administration

    Oral gavage

Customer Product Validation

Data from [Proc Natl Acad Sci U S A, 2014, 111(12), E1140-8]

Data from [Data independently produced by Am J Respir Cell Mol Biol, 2014, 50(1), 170-9]

Data from [Data independently produced by , , Cancer Res, 2017, 77(9):2413-2423]

Data from [Data independently produced by , , Respir Res, 2017, 18(1):111]

Selleck's GSK429286A has been cited by 24 publications

Chemically induced revitalization of damaged hepatocytes for regenerative liver repair [ iScience, 2023, 26(12):108532] PubMed: 38144457
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] PubMed: 33067904
Complementary roles of platelet αIIbβ3 integrin, phosphatidylserine exposure and cytoskeletal rearrangement in the release of extracellular vesicles [ Atherosclerosis, 2020, 310:17-25] PubMed: 32877806
The TGF-b/SOX4 axis and ROS-driven autophagy co-mediate CD39 expression in regulatory T-cells. [ FASEB J, 2020, 22] PubMed: 32319705
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
A Combined Approach Reveals a Regulatory Mechanism Coupling Src's Kinase Activity, Localization, and Phosphotransferase-Independent Functions. [ Mol Cell, 2019, 74(2):393-408] PubMed: 30956043
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] PubMed: 30760778
Rho-associated kinase and zipper-interacting protein kinase, but not myosin light chain kinase, are involved in the regulation of myosin phosphorylation in serum-stimulated human arterial smooth muscle cells [ PLoS One, 2019, 14(12):e0226406] PubMed: 31834925
Fibronectin regulates the self-renewal of rabbit limbal epithelial stem cells by stimulating the Wnt11/Fzd7/ROCK non-canonical Wnt pathway [ Exp Eye Res, 2019, 185:107681] PubMed: 31150636

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.