2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton MAPK/ERK Pathway
  3. ROCK Ribosomal S6 Kinase (RSK)
  4. GSK-25

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).

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

GSK-25 Chemical Structure

GSK-25 Chemical Structure

CAS No. : 874119-56-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 119 In-stock
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 105 In-stock
10 mg USD 178 In-stock
25 mg USD 255 In-stock
50 mg USD 390 In-stock
100 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK-25 Related Antibodies

Top Publications Citing Use of Products

View All ROCK Isoform Specific Products:

View All Isoforms
ROCK ROCK1 ROCK2

View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

View All Isoforms
p70S6K RSK1 RSK2 RSK3 RSK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].

IC50 & Target[1]

ROCK1

7 nM (IC50)

RSK1

398 nM (IC50)

p70S6K

1000 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
6 nM
Compound: 25
Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA
Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA
[PMID: 18842034]
In Vivo

GSK-25 (Rat aorta IC50=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure[1].
GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey)[1].

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

513.33

Formula

C24H16Cl2F2N6O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC(C2=NC(C3=C(F)C=C(Cl)C=C3)C(C(NC4=C(F)C=C(NN=C5)C5=C4)=O)=C(C)N2)=CC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (97.40 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 1.9481 mL 9.7403 mL 19.4806 mL
5 mM 0.3896 mL 1.9481 mL 3.8961 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (5.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.87 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:

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: 99.68%

SDS (393 KB)

COA (253 KB) HNMR (202 KB) LCMS (120 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, 6 months; -20°C, 1 month. 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 1.9481 mL 9.7403 mL 19.4806 mL 48.7016 mL
5 mM 0.3896 mL 1.9481 mL 3.8961 mL 9.7403 mL
10 mM 0.1948 mL 0.9740 mL 1.9481 mL 4.8702 mL
15 mM 0.1299 mL 0.6494 mL 1.2987 mL 3.2468 mL
20 mM 0.0974 mL 0.4870 mL 0.9740 mL 2.4351 mL
25 mM 0.0779 mL 0.3896 mL 0.7792 mL 1.9481 mL
30 mM 0.0649 mL 0.3247 mL 0.6494 mL 1.6234 mL
40 mM 0.0487 mL 0.2435 mL 0.4870 mL 1.2175 mL
50 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9740 mL
60 mM 0.0325 mL 0.1623 mL 0.3247 mL 0.8117 mL
80 mM 0.0244 mL 0.1218 mL 0.2435 mL 0.6088 mL
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GSK-25 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:

GSK-25874119-56-9GSK25GSK 25ROCKRibosomal S6 Kinase (RSK)Rho-associated protein kinaseRho-associated kinaseRho-kinaseROKS6Kselectiveorallybioavailablep70S6KP450bloodpressureInhibitorinhibitorinhibit

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