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ROCK2-IN-14
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Catalog No. T217783 Copy Product Info
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ROCK2-IN-14 is an orally bioavailable and selective ROCK2 inhibitor with an IC50 of 4.8 nM, and it is 212 times more selective for ROCK2 over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 reduces S100A9 expression, inhibits NM2 phosphorylation, and corrects cytoskeletal abnormalities. Consequently, it lowers levels of inflammatory cytokines, alleviates skin inflammation, and exhibits anti-inflammatory effects. In atopic dermatitis (AD) mouse models, ROCK2-IN-14 significantly reduces ear thickening and decreases IgE, TNF-α, IL-6, and TSLP levels. The compound demonstrates good safety, with a maximum tolerable oral dose exceeding 500 mg/kg, making it a potential candidate for atopic dermatitis research.
ROCK2-IN-14
Cas No. 3115784-59-0
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | ROCK2-IN-14 is an orally bioavailable and selective ROCK2 inhibitor with an IC50 of 4.8 nM, and it is 212 times more selective for ROCK2 over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 reduces S100A9 expression, inhibits NM2 phosphorylation, and corrects cytoskeletal abnormalities. Consequently, it lowers levels of inflammatory cytokines, alleviates skin inflammation, and exhibits anti-inflammatory effects. In atopic dermatitis (AD) mouse models, ROCK2-IN-14 significantly reduces ear thickening and decreases IgE, TNF-α, IL-6, and TSLP levels. The compound demonstrates good safety, with a maximum tolerable oral dose exceeding 500 mg/kg, making it a potential candidate for atopic dermatitis research. |
| Targets & IC50 | ROCK2:4.8 nM |
| In vitro | ROCK2-IN-14 (compound 10d) within a range of 10 nM to 1 μM for 24 hours significantly suppresses the protein expression levels of S100A9, p-MYPT1, and p-NM2 in HaCaT cells. At the same concentration range for 48 hours, it reduces the mRNA expression levels of IL-6 and TSLP in a concentration-dependent manner. Additionally, after 24 hours, ROCK2-IN-14 significantly ameliorates abnormal accumulation of cytoskeletal F-actin in HaCaT cells as observed in immunofluorescence experiments. Furthermore, at concentrations from 1 nM to 1 μM for 72 hours, ROCK2-IN-14 shows no significant impact on the viability of HaCaT cells, with cell survival rates exceeding 90% across all groups. When applied at 1 μM for 24 hours, the compound markedly reduces cell migration ability, with the scratch wound healing rate decreasing by approximately 45% compared to the control group. |
| In vivo | ROCK2-IN-14 (compound 10d), administered orally at doses of 10 mg/kg, 30 mg/kg, and 100 mg/kg once daily for 14 days, significantly reduces ear swelling in atopic dermatitis (AD) model BALB/c mice, and decreases serum levels of IgE, TNF-α, IL-6, and TSLP. Additionally, a single oral dose of ROCK2-IN-14 at 500 mg/kg in ICR mice shows no evident toxicity, with a survival rate of 100%, and a maximum tolerated dose exceeding 500 mg/kg. |
| Molecular Weight | 434.55 |
| Formula | C24H26N4O2S |
| Cas No. | 3115784-59-0 |
| Smiles | O=C(NCC=1C=CC=C(OCCCN(C)C)C1)C=2SC3=CC(=CC=C3C2)C=4C=NNC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: ROCK2-IN-14 in vivo | ROCK2-IN-14 in vitro | ROCK2-IN-14 formula | ROCK2-IN-14 molecular weight
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