Art. -Nr.: HY-15556

GSK269962A

Name: GSK269962A
Brand: MedChemExpress
SKU: HY-15556
Price: 106.00 USD
Availability: InStock
Rating: 5 (6 reviews)

(Synonyms: GSK 269962)

6 Cited Publications

Kundenbewertung

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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Reinheit : 99.75%
CAS. Nr.: 850664-21-0
Formel: C₂₉H₃₀N₈O₅
Molecular Weight:570.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK269962A Chemical Structure

CAS. Nr.: 850664-21-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle ROCK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	1.6 nM Compound: GSK 269962	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	[PMID: 31330446]
Sf9	IC₅₀	1.6 nM Compound: GSK269962A	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	[PMID: 17018693]
Sf9	IC₅₀	1.8 nM Compound: 6n	Inhibition of human ROCK1 in Sf9 cells Inhibition of human ROCK1 in Sf9 cells	[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].
? 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.

In Vivo

GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Sprague-Dawley rats (350-400g)^[1]
Dosage:

0.3, 1, and 3 mg/kg
Administration:

Oral gavage; 12 hours
Result:

Induced a dose-dependent reduction in blood pressure.

Related Protocols :

Research Protocol for Inflammation-related Diseases

Chemical Information

CAS. Nr. 850664-21-0
Appearance Solid
Molecular Weight 570.60
Formel C₂₉H₃₀N₈O₅
Color White to light yellow
SMILES

CCN1C2=CC(OC3=CC=CC(NC(C4=CC=C(OCCN5CCOCC5)C=C4)=O)=C3)=NC=C2N=C1C6=NON=C6N
Synonyms

GSK 269962
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All Cell Proliferation/Viability AssayRT-PCRFlow CytometryMicrobiological AssayWB

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Journal Impact Factor

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

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
Virology

The actin cytoskeleton is important for pseudorabies virus infection. [Abstract]

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.
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.
bioRxiv

2025 April 25.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7525 mL

8.7627 mL

17.5254 mL

5 mM

0.3505 mL

1.7525 mL

3.5051 mL

10 mM

0.1753 mL

0.8763 mL

1.7525 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Doe C, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

GSK269962A

6 Cited Publications

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GSK269962A

Publications Citing Use of MedChemExpress (MCE) GSK269962A

Alle ROCK Isoform-spezifische Produkte anzeigen