2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. GSK269962A

GSK269962A  (Synonyms: GSK 269962)

Cat. No.: HY-15556 Purity: 99.83%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

GSK269962A Chemical Structure

GSK269962A Chemical Structure

CAS No. : 850664-21-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 133 In-stock
Solution
10 mM * 1 mL in DMSO USD 133 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 106 In-stock
10 mg USD 150 In-stock
50 mg USD 480 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 3 publication(s) in Google Scholar

Other Forms of GSK269962A:

GSK269962A Related Antibodies

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ROCK ROCK1 ROCK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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)

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.

GSK269962A Related Antibodies
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.
Molecular Weight

570.60

Formula

C29H30N8O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7525 mL 8.7627 mL 17.5254 mL
5 mM 0.3505 mL 1.7525 mL 3.5051 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.83%

COA (251 KB) LCMS (264 KB)

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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GSK269962A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK269962A850664-21-0GSK 269962GSK269962GSK-269962ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK1ROCK2anti-inflammatoryvasodilatorycardiovascularantihypertensivebloodpressureInhibitorinhibitorinhibit

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