ROCK2-IN-17
ROCK2-IN-17 is an orally active and selective ROCK2 inhibitor with an IC50 of 8.1 nM. ROCK2-IN-17 achieves its antifibrotic effect by inhibiting the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-17 can be used for pulmonary fibrosis research.
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- 화학식: C24H18FN9O2
- 분자량:483.46
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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 8.1 nM (IC50) |
STAT3 |
In Vitro
ROCK2-IN-17 (Compound 39) exhibits an IC50 of 1.4 μM against ROCK1, a ROCK1/ROCK2 selectivity index of 200, and demonstrates ROCK2 selectivity in a screen of 81 kinases at a concentration of 1 μM[1].
ROCK2-IN-17 (2.5-10 μM; 48 h) suppresses TGF-β1-induced fibroblast activation in NIH-3T3 and MRC-5 cells[1].
ROCK2-IN-17 (5 μM; 24 h) inhibits TGF-β1-induced NIH-3T3 fibroblast migration in wound healing and transwell migration assays[1].
ROCK2-IN-17 (0-10 μM) dose-dependently reduces p-STAT3, p-Smad2/3 and α-SMA expression in TGF-β1-stimulated NIH-3T3 and MRC-5 fibroblasts, indicating inhibition of the ROCK2/STAT3 and TGF-β/Smad signaling pathways[1].
ROCK2-IN-17 (0.37-30 μM) shows weak inhibitory activity against hERG channels in automated patch-clamp assays, inhibiting them by only 11.4% at a concentration of 30 μM, with an hERG IC50 > 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NIH-3T3
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Suppressed TGF-β1-induced fibroblast activation in a dose-dependent manner.
Reduced the TGF-β1-induced increase in NIH-3T3 cell viability, indicating antifibrotic activity in fibroblasts.
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Cell Line:MRC-5
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Suppressed TGF-β1-induced fibroblast activation in a dose-dependent manner.
Reduced the TGF-β1-induced increase in MRC-5 cell viability, supporting its antifibrotic effect in human lung fibroblasts.
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Cell Line:NIH-3T3
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Concentration:5 μM
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Incubation Time:24 h
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Result:Reduced TGF-β1-induced wound closure in NIH-3T3 cells.
TGF-β1 increased the wound closure rate from 25.7% to 51.7%, while compound administration effectively attenuated this migration-promoting effect.
Reduced the number of TGF-β1-induced migrating NIH-3T3 cells in the transwell assay, confirming inhibition of fibroblast migration.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice challenged with Bleomycin (4 U/kg) by intratracheal administration on day 1[1]
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Dosage:50, 100 mg/kg
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Administration:Oral gavage (p.o.); once daily; for 14 days
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Result:Attenuated bleomycin-induced pulmonary fibrosis in vivo.
Improved body weight changes and reduced hydroxyproline content in lung homogenates, indicating decreased collagen deposition.
Mitigated alveolar structural distortion, dense extracellular matrix fiber formation, lung parenchymal thickening, collagen deposition and inflammatory cell infiltration according to H&E and Masson staining.
Reduced α-SMA fluorescence intensity in lung tissues according to immunofluorescence staining.
Dose-dependently downregulated the mRNA expression of α-SMA, COL1A1 and fibronectin in lung tissues.
Showed no obvious pathological abnormalities in heart, liver, spleen or kidney sections after 14 days of administration.
Chemical Information
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분자량 483.46
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화학식 C24H18FN9O2
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SMILES
C[C@@H](C1=NC(C2=CN=C3C=CC(NC4=CC=C5C(C=NN5)=C4)=NN32)=NO1)NC(C6=CC=C(C=C6)F)=O
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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-17 Related Classifications
HY-184149 Related Classifications
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Keywords
- ROCK2-IN-17
- ROCK
- TGF-beta/Smad
- STAT
- Rho-associated protein kinase
- Rho-associated kinase
- Rho-kinase
- ROK
- Transforming growth factor beta
- ROCK2 inhibitor
- selective
- orally active
- ROCK1 selectivity
- TGF-β/Smad signaling pathway
- ROCK2/STAT3 signaling pathway
- fibroblast activation
- fibroblast migration
- α-SMA
- COL1A1
- fibronectin
- hydroxyproline
- bleomycin-induced pulmonary fibrosis model
- NIH-3T3
- MRC-5
- C57BL/6 mouse
- pulmonary fibrosis
- Inhibitor
- inhibitor
- inhibit