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

For research use only. We do not sell to patients.

ROCK2-IN-10

ROCK2-IN-10 Chemical Structure

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ROCK2-IN-10 Related Antibodies

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ROCK ROCK1 ROCK2

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target[1]

ROCK2

0.020 μM (IC50)

ROCK1

0.821 μM (IC50)

In Vitro

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.

ROCK2-IN-10 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 and 5 μM
Incubation Time: 24 h
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.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 and 5 μM
Incubation Time: 0, 24 and 48 h
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 %.
Molecular Weight

582.70

Formula

C32H38N8O3
SMILES

CC(C=C1)=CC=C1NC(OC[C@H](CCC2)N2C3=NC(NC4=CC5=C(C=C4)NN=C5)=CC=C3NC(CNC6CCCC6)=O)=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-10 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-10ROCKSTATRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK2cytoskeletal organizationMDA-MB-231 cellsmetastasisSTAT3breast cancerInhibitorinhibitorinhibit

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