2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton JAK/STAT Signaling
  3. ROCK TGF-beta/Smad STAT
  4. 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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ROCK2-IN-17

ROCK2-IN-17 Chemical Structure

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ROCK2-IN-17 Related Antibodies

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ROCK ROCK1 ROCK2

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

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.

ROCK2-IN-17 Related Antibodies

Cell Viability Assay

Cell Line: NIH-3T3
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
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.

Cell Viability Assay

Cell Line: MRC-5
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
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.

Cell Migration Assay

Cell Line: NIH-3T3
Concentration: 5 μM
Incubation Time: 24 h
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
Species Dose Route AUC0-t AUC0-∞ Tmax T1/2 Cmax CL Vz F
Rat[1] 10 mg/kg i.v. 3176.0 h·μg/L 3221.5 h·μg/L 0.083 h 5.5 h 2246.5 μg/L 3.2 L/h/kg 25.3 L/kg /
Rat[1] 20 mg/kg p.o. 1687.7 h·μg/L 1747.2 h·μg/L 0.9 h 5 h 306.8 μg/L 4.5 L/h/kg 33.6 L/kg 36.2 %
In Vivo

ROCK2-IN-17 (Compound 39) (50, 100 mg/kg; p.o.; once daily; for 14 days) attenuates Bleomycin (HY-108345) -induced pulmonary fibrosis in mouse model[1].

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

Animal Model: Male C57BL/6 mice challenged with Bleomycin (4 U/kg) by intratracheal administration on day 1[1]
Dosage: 50, 100 mg/kg
Administration: Oral gavage (p.o.); once daily; for 14 days
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.
Molecular Weight

483.46

Formula

C24H18FN9O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ROCK2-IN-17 Related Classifications

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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:

ROCK2-IN-17ROCKTGF-beta/SmadSTATRho-associated protein kinaseRho-associated kinaseRho-kinaseROKTransforming growth factor betaROCK2 inhibitorselectiveorally activeROCK1 selectivityTGF-β/Smad signaling pathwayROCK2/STAT3 signaling pathwayfibroblast activationfibroblast migrationα-SMACOL1A1fibronectinhydroxyprolinebleomycin-induced pulmonary fibrosis modelNIH-3T3MRC-5C57BL/6 mousepulmonary fibrosisInhibitorinhibitorinhibit

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