GSK429286A
Based on 9 publication(s) in Google Scholar
GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
For research use only. We do not sell to patients.
- Purity: 98.27%
- CAS No.: 864082-47-3
- Formula: C21H16F4N4O2
- Molecular Weight:432.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK429286A
More- Nat Immunol. 2024 Apr;25(4):659-670. [Abstract]
- Acta Pharmacol Sin. 2024 Jul;45(7):1477-1491. [Abstract]
- Clin Transl Med. 2022 Oct;12(10):e1036. [Abstract]
- Commun Biol. 2023 Nov 18;6(1):1176. [Abstract]
- J Cell Sci. 2025 Sep 16:jcs.264193. [Abstract]
- Mol Hum Reprod. 2023 Apr 29;29(5):gaad010. [Abstract]
- Virology. 2024 Dec:600:110233. [Abstract]
- Authorea. 2022 Nov 4.
- Patent. US20180263995A1.
Biological Activity
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ROCK1 14 nM (IC50) |
RSK 780 nM (IC50) |
p70S6K 1940 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
14 nM
Compound: 15
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Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM
Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM
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[PMID: 17201405] |
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). 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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 864082-47-3
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Appearance Solid
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Molecular Weight 432.37
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Formula C21H16F4N4O2
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Color White to off-white
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SMILES
O=C(C(C(C1=CC=C(C(F)(F)F)C=C1)C2)=C(C)NC2=O)NC3=CC4=C(NN=C4)C=C3F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Immunol
2024 Apr;25(4):659-670. PMID: 38499799 -
Acta Pharmacol Sin
2024 Jul;45(7):1477-1491. PMID: 38538716 -
Clin Transl Med
Inhibition of ROCK ameliorates pulmonary fibrosis by suppressing M2 macrophage polarisation through phosphorylation of STAT3. [Abstract]2022 Oct;12(10):e1036. PMID: 36178087 -
Commun Biol
Selectivity matters: selective ROCK2 inhibitor ameliorates established liver fibrosis via targeting inflammation, fibrosis, and metabolism. [Abstract]2023 Nov 18;6(1):1176. PMID: 37980369 -
J Cell Sci
2025 Sep 16:jcs.264193. PMID: 40955174 -
Mol Hum Reprod
Semaphorin 4C regulates ovarian steroidogenesis through RHOA/ROCK1-mediated actin cytoskeleton rearrangement. [Abstract]2023 Apr 29;29(5):gaad010. PMID: 36892447 -
Virology
2024 Dec:600:110233. PMID: 39255726 -
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Solvent & Solubility
DMSO : ≥ 51 mg/mL (117.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats: Spontaneously hypertensive rats (SHRs) are treated with GSK429286A to establish its effect on mean arterial pressure. Compound is administered by single dose oral gavage (3, 10, 30 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9. [Content Brief]
[2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3128 mL | 11.5642 mL | 23.1283 mL | 57.8208 mL |
| 5 mM | 0.4626 mL | 2.3128 mL | 4.6257 mL | 11.5642 mL | |
| 10 mM | 0.2313 mL | 1.1564 mL | 2.3128 mL | 5.7821 mL | |
| 15 mM | 0.1542 mL | 0.7709 mL | 1.5419 mL | 3.8547 mL | |
| 20 mM | 0.1156 mL | 0.5782 mL | 1.1564 mL | 2.8910 mL | |
| 25 mM | 0.0925 mL | 0.4626 mL | 0.9251 mL | 2.3128 mL | |
| 30 mM | 0.0771 mL | 0.3855 mL | 0.7709 mL | 1.9274 mL | |
| 40 mM | 0.0578 mL | 0.2891 mL | 0.5782 mL | 1.4455 mL | |
| 50 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 1.1564 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3855 mL | 0.9637 mL | |
| 80 mM | 0.0289 mL | 0.1446 mL | 0.2891 mL | 0.7228 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2313 mL | 0.5782 mL |
GSK429286A Related Classifications
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