ROCK2-IN-10
ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research.
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- Fòrmula: C32H38N8O3
- Peso molecular:582.70
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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ROCK2 0.020 μM (IC50) |
ROCK1 0.821 μM (IC50) |
ROCK2-IN-10 (compound S9) derives its excellent potency against ROCK2 from the hydrogen bonds formed by its acetylamino chain with Asp218 and Asn219[1].
ROCK2-IN-10 (5 μM, 24 h) disrupts the overall morphology of MDA-MB-231 cells, resulting in blunted filopodia and discontinuous F-actin stress fibers along the cell contour[1].
ROCK2-IN-10 (2.5-5 μM, 0-48 h) exhibits potent, dose-dependent inhibition of cell migration in MDA-MB-231 cells, and demonstrates significantly greater efficacy than Belumosudil (HY-15307) at both 24 h and 48 h[1].
ROCK2-IN-10 (2.5-5 μM, 24 h) downregulates phosphorylation of STAT3 in a dose-dependent manner, contributing to a promising anti-metastasis efficacy against MDA-MB-231 cells[1].
ROCK2-IN-10 (72 h) exhibits minimal cytotoxicity in MDA-MB-231 cells with an IC50 of 12.77 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5 and 5 μM
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Incubation Time:24 h
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Result:Decreased p-STAT3 to nearly half of the control group at the concentration of 5 μM.
Reduced p-STAT3 levels in MDA-MB-231 cells in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5 and 5 μM
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Incubation Time:0, 24 and 48 h
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Result:Inhibited the migration of MDA-MB-231 cells, reducing wound closure to 9.65 % after 24 h, compared to 24.51 % in the control group.
Exhibited stronger inhibition than Belumosudil at 5 μM after 24 h, with cell migration rates of 3.48 % compared to 4.74 %.
Maintained a more prominent anti-metastatic effect than Belumosudil at 5 μM after 48 h, with cell migration rates of 9.33 % compared to 12.43 %.
Chemical Information
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Peso molecular 582.70
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Fòrmula C32H38N8O3
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SMILES
CC(C=C1)=CC=C1NC(OC[C@H](CCC2)N2C3=NC(NC4=CC5=C(C=C4)NN=C5)=CC=C3NC(CNC6CCCC6)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ROCK2-IN-10 Related Classifications
HY-175843 Related Classifications
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