GSK269962A
Based on 6 publication(s) in Google Scholar
GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities.
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- Purity : 99.75%
- CAS No.: 850664-21-0
- 화학식: C29H30N8O5
- 분자량:570.60
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK269962A
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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
제품 설명
IC50 & Target
[1]|
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) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
1.6 nM
Compound: GSK 269962
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Inhibition of N-terminal His-tagged human ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as substrate incubated for 90 mins in presence of [gamma33P]ATP by scintillation counting method
Inhibition of N-terminal His-tagged human ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as substrate incubated for 90 mins in presence of [gamma33P]ATP by scintillation counting method
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[PMID: 31330446] |
| Sf9 | IC50 |
1.6 nM
Compound: GSK269962A
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Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
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[PMID: 17018693] |
| Sf9 | IC50 |
1.8 nM
Compound: 6n
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Inhibition of human ROCK1 in Sf9 cells
Inhibition of human ROCK1 in Sf9 cells
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[PMID: 17201404] |
In Vitro
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].
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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. Further protocols information, click here.
In Vivo
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. 850664-21-0
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Appearance Solid
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분자량 570.60
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화학식 C29H30N8O5
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Color 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
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Synonyms
GSK 269962
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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 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 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 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 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 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 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 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 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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용액&용해도
In Vitro:
DMSO : 100 mg/mL (175.25 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.5 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
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Data Sheet (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7525 mL | 8.7627 mL | 17.5254 mL | 43.8135 mL |
| 5 mM | 0.3505 mL | 1.7525 mL | 3.5051 mL | 8.7627 mL | |
| 10 mM | 0.1753 mL | 0.8763 mL | 1.7525 mL | 4.3814 mL | |
| 15 mM | 0.1168 mL | 0.5842 mL | 1.1684 mL | 2.9209 mL | |
| 20 mM | 0.0876 mL | 0.4381 mL | 0.8763 mL | 2.1907 mL | |
| 25 mM | 0.0701 mL | 0.3505 mL | 0.7010 mL | 1.7525 mL | |
| 30 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4605 mL | |
| 40 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL | |
| 50 mM | 0.0351 mL | 0.1753 mL | 0.3505 mL | 0.8763 mL | |
| 60 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7302 mL | |
| 80 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5477 mL | |
| 100 mM | 0.0175 mL | 0.0876 mL | 0.1753 mL | 0.4381 mL |
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