ROCK2-IN-14
ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 can be used for research on atopic dermatitis.
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- CAS No.: 3115784-59-0
- 화학식: C24H26N4O2S
- 분자량:434.55
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
ROCK2 4.8 nM (IC50) |
In Vitro
ROCK2-IN-14 (compound 10d) (10 nM-1 μM; 24 h) significantly inhibits the protein expression levels of S100A9, p-MYPT1 and p-NM2 in HaCaT cells[1].
ROCK2-IN-14 (10 nM-1 μM; 48 h) reduces the mRNA expression levels of IL-6 and TSLP in HaCaT cells in a concentration-dependent manner[1].
ROCK2-IN-14 (10 nM-1 μM; 24 h) significantly ameliorates the abnormal polymerization of cytoskeletal F-actin in HaCaT cells, as observed by IF assays[1].
ROCK2-IN-14 (1 nM-1 μM; 72 h) exerts no significant effect on the viability of HaCaT cells, with the cell survival rate of all groups being higher than 90%[1].
ROCK2-IN-14 (1 μM; 24 h) significantly reduces the migratory capacity of HaCaT cells, with the scratch wound healing rate decreasing by approximately 45% compared with the control group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM
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Incubation Time:72 h
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Result:Did not significantly affect the viability of HaCaT cells, and the cell survival rate was higher than 90% at all tested concentrations.
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Cell Line:HaCaT
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Concentration:10 nM, 100 nM, 1 μM
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Incubation Time:48 h
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Result:Reduced the mRNA expression levels of inflammatory factors IL-6 and TSLP in a concentration-dependent manner, with the most significant reduction at 1 μM (by 68% and 72%, respectively).
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Cell Line:HaCaT
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Concentration:48 h
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Incubation Time:24 h
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Result:Significantly downregulated the protein expression levels of S100A9, p-MYPT1 (Thr853), and p-NM2 in HaCaT cells in a concentration-dependent manner.
Parmacokinetics
In Vivo
ROCK2-IN-14 (compound 10d) (dose: 500 mg/kg; administration route: oral gavage; administration frequency: single dose; administration cycle: 1 time) shows no obvious toxic reactions in the acute toxicity model of ICR mice, with a 100% survival rate of mice and a maximum tolerated dose exceeding 500 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, 18-22 g, 6-8 weeks old) + Atopic Dermatitis (AD) model[1]
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Dosage:10 mg/kg (0.5% CMC-Na), 30 mg/kg (0.5% CMC-Na), 100 mg/kg (0.5% CMC-Na)
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Administration:14 consecutive days of oral gavage administration once daily
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Result:Significantly reduced the ear thickness increase of AD model mice by 35% (10 mg/kg), 58% (30 mg/kg) and 72% (100 mg/kg), compared with the model group; serum levels of IgE, TNF-α, IL-6 and TSLP were decreased by 28%, 42%, 51% and 48% at 30 mg/kg dosage, respectively.
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Animal Model:ICR mice (male and female, 20-24 g, 7-9 weeks old) + Acute toxicity model[1]
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Dosage:500 mg/kg
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Administration:single oral gavage administration
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Result:No obvious toxic symptoms (such as weight loss, abnormal behavior, organ damage) were observed in mice within 14 days of observation, and the survival rate of mice was 100%, indicating that the maximum tolerated dose (MTD) was more than 500 mg/kg.
- Kinase activity and phosphorylation assays
- RNA extraction experimental
- Western Blot
- Imiquimod-Induced Psoriasiform Dermatitis
- Cotton Pellet Granuloma
- Carrageenan-Induced Paw Edema
- TPA/Croton Oil Ear Edema and Dermatitis
- Contact Hypersensitivity Dermatitis
- Protocol for Kinase activity and phosphorylation assays
- Research Protocol for Inflammation-related Diseases
- Phalloidin F-actin cytoskeleton staining
- How to Choose the Right Model Animal
Chemical Information
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CAS No. 3115784-59-0
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분자량 434.55
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화학식 C24H26N4O2S
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SMILES
CN(C)CCCOC1=CC(CNC(C2=CC3=CC=C(C4=CNN=C4)C=C3S2)=O)=CC=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ROCK2-IN-14 Related Classifications
HY-181576 Related Classifications
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