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

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.

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

Rho-Kinase-IN-2 Chemical Structure

Rho-Kinase-IN-2 Chemical Structure

CAS No. : 2573071-18-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Rho-Kinase-IN-2 Related Antibodies

Top Publications Citing Use of Products

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ROCK ROCK1 ROCK2

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  • Purity & Documentation

  • References

  • Customer Review

Description

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research[1].

IC50 & Target

ROCK2

3 nM (IC50)

In Vitro

Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation[1].

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

Rho-Kinase-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: A7r5 and PANC1 cells
Concentration: 0-10 mM
Incubation Time: 1 hour
Result: Showed concentration-dependent effects, leading to an increase in AKT phosphorylation (EC50=28 nM) and a decrease in MYPT1 phosphorylation (IC50=14 nM).
In Vivo

Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment[1].
Rho-Kinase-IN-2 (oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate[1].
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations[1].

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

Animal Model: Male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h
Result: Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC50=∼6 nM.
Animal Model: 3−4 months old heterozygote Q175DN KI and wild-type littermate mice[1]
Dosage: 10 or 20 mg/kg
Administration: Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks
Result: Scored neurological index normally at all doses although a slight loss in bodyweight (∼2%) in the 20 mg/kg treatment group.
Animal Model: Heterozygote HTT zQ175DN knock-in mice[1]
Dosage: 1-20 mg/kg
Administration: Oral adiministration; 1-20 mg/kg; once
Result: Remained over MYPT1 IC50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing.
Animal Model: CD1 mice[1]
Dosage: 10 and 20 mg/kg
Administration: Oral adiministration; 10 or 20 mg/kg; once
Result: Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ∼0.5 to 2 h post dose.
Animal Model: Heterozygote Q175DN KI mouse model of HD[1]
Dosage: 10 mg/kg
Administration: Oral adiministration; 10 mg/kg; twice a day; 90 days
Result: Led to lower-than-expected brain concentrations compared to single dosing.
Molecular Weight

372.44

Formula

C20H25FN4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1[C@H](C)CN(C2=C(F)C=NC=C2)CC1)N[C@@H](C3=CC=CC(OC)=C3)C
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 (134.25 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 2.6850 mL 13.4250 mL 26.8500 mL
5 mM 0.5370 mL 2.6850 mL 5.3700 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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
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 2.6850 mL 13.4250 mL 26.8500 mL 67.1249 mL
5 mM 0.5370 mL 2.6850 mL 5.3700 mL 13.4250 mL
10 mM 0.2685 mL 1.3425 mL 2.6850 mL 6.7125 mL
15 mM 0.1790 mL 0.8950 mL 1.7900 mL 4.4750 mL
20 mM 0.1342 mL 0.6712 mL 1.3425 mL 3.3562 mL
25 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6850 mL
30 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2375 mL
40 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6781 mL
50 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
60 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
80 mM 0.0336 mL 0.1678 mL 0.3356 mL 0.8391 mL
100 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
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Rho-Kinase-IN-2 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:

Rho-Kinase-IN-22573071-18-6ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKHuntington’sA7r5PANC1Inhibitorinhibitorinhibit

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