GSK269962A hydrochloride
Based on 6 publication(s) in Google Scholar
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 2095432-71-4
- Formula: C29H31ClN8O5
- Molecular Weight:607.06
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK269962A hydrochloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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RT-PCR
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Microbiological Assay
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WB
Biological Activity
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ROCK1 1.6 nM (IC50) |
ROCK2 4 nM (IC50) |
RSK1 132 nM (IC50) |
MSK1 49 nM (IC50) |
AKT1 955 nM (IC50) |
AKT2 1350 nM (IC50) |
AKT3 1510 nM (IC50) |
CDK2 3500 nM (IC50) |
GSK3α 1260 nM (IC50) |
GSK269962A has an IC50 of 1.6 nM toward recombinant human ROCK1. GSK269962A exhibits more than 30-fold selectivity against a panel of serine/threonine kinases[1].
GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM[1].
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.
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Animal Model:Male Sprague-Dawley rats (350-400g)[1]
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Dosage:0.3, 1, and 3 mg/kg
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Administration:Oral gavage; 12 hours
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Result:Induced a dose-dependent reduction in blood pressure.
Chemical Information
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CAS No. 2095432-71-4
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Appearance Solid
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Molecular Weight 607.06
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Formula C29H31ClN8O5
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Color Off-white to light yellow
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SMILES
CCN1C2=CC(OC3=CC=CC(NC(C4=CC=C(OCCN5CCOCC5)C=C4)=O)=C3)=NC=C2N=C1C6=NON=C6N.Cl
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Synonyms
GSK 269962 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Int Immunopharmacol
A multi-omics R-loop-linked risk program highlights CKS2-positive proliferative tumor cells as drivers of glioma growth. [Abstract]2026 Apr 15:175:116421. PMID: 41763168 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Virology
2024 Dec:600:110233. PMID: 39255726
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2024 Dec:600:110233. [Abstract]
CCK-8 cell viability assay in PK-15 cells after treatment with GSK269962A (10-5000 nM; 24 h). GSK269962A did not exhibit cytotoxicity in PK-15 cells over the tested concentration range.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2024 Dec:600:110233. [Abstract]
Flow cytometric analysis of GFP fluorescence in PK-15 cells pretreated with GSK269962A (10-5000 nM) for 4 h, followed by PRV-GFP infection for 24 h in the continued presence of GSK269962A. GSK269962A inhibited PRV infection in PK-15 cells.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2024 Dec:600:110233. [Abstract]
PRV gB and TK mRNA levels in PK-15 cells after 4 h of pretreatment with GSK269962A (10-500 nM), followed by PRV-QXX infection for 24 h in the continued presence of GSK269962A. GSK269962A dose-dependently reduced PRV gB and TK mRNA levels.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2024 Dec:600:110233. [Abstract]
PRV titers in PK-15 cells after 4 h of pretreatment with GSK269962A (10-500 nM), followed by PRV-QXX infection for 24 h in the continued presence of GSK269962A, as determined by the PFU assay. GSK269962A reduced progeny PRV titers.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2024 Dec:600:110233. [Abstract]
Western blot analysis of PRV gB protein in PK-15 cells after 4 h of pretreatment with GSK269962A (10-500 nM), followed by PRV-QXX infection for 24 h in the continued presence of GSK269962A. PRV gB protein expression was decreased due to the treatment of GSK269962A.
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Virology
Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]2023 Aug:585:205-214. PMID: 37384967
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2023 Aug:585:205-214. [Abstract]
EV-A71 viral mRNA from RD cells after treatment with GSK269962A (10 μM; 48 h), as measured by RT-qPCR. GSK269962A was used as a positive control.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2023 Aug:585:205-214. [Abstract]
Viral titers in culture supernatants from EV-A71-infected RD cells after treatment with GSK269962A (10 μM; 48 h), as determined by the TCID50 assay. GSK269962A was used as a positive control.
GSK269962A hydrochloride purchased from MedChemExpress. Usage Cited in: Virology. 2023 Aug:585:205-214. [Abstract]
Western blot analysis of the EV-A71 structural protein VP1 in infected RD cells after treatment with GSK269962A (10 μM; 48 h). GSK269962A was used as a positive control.
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Solvent & Solubility
DMSO : 100 mg/mL (164.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 5 mg/mL (8.24 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (8.24 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6473 mL | 8.2364 mL | 16.4728 mL | 41.1821 mL |
| 5 mM | 0.3295 mL | 1.6473 mL | 3.2946 mL | 8.2364 mL | |
| 10 mM | 0.1647 mL | 0.8236 mL | 1.6473 mL | 4.1182 mL | |
| 15 mM | 0.1098 mL | 0.5491 mL | 1.0982 mL | 2.7455 mL | |
| 20 mM | 0.0824 mL | 0.4118 mL | 0.8236 mL | 2.0591 mL | |
| 25 mM | 0.0659 mL | 0.3295 mL | 0.6589 mL | 1.6473 mL | |
| 30 mM | 0.0549 mL | 0.2745 mL | 0.5491 mL | 1.3727 mL | |
| 40 mM | 0.0412 mL | 0.2059 mL | 0.4118 mL | 1.0296 mL | |
| 50 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8236 mL | |
| 60 mM | 0.0275 mL | 0.1373 mL | 0.2745 mL | 0.6864 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2059 mL | 0.5148 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1647 mL | 0.4118 mL |
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