ROCK2-IN-19
ROCK2-IN-19, the non-isotopic form of compound 22d, is an orally active and selective ROCK2 inhibitor with an IC50 value of 13 nM. ROCK2-IN-19 selectively inhibits the phosphorylation of STAT3 at tyrosine 705, and suppresses breast cancer metastasis by disrupting the ROCK2-STAT3 signaling axis. ROCK2-IN-19 exhibits anti-metastatic activity in both cancer cells and xenograft models. ROCK2-IN-19 can be used in breast cancer-related research.
For research use only. We do not sell to patients.
- Formula: C25H22N4O3
- Molecular Weight:426.47
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ROCK2 13 nM (IC50) |
STAT3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
14.48 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
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42593922 |
| HUVEC | IC50 |
51.19 μM
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Antiproliferative activity against HUVEC cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
Antiproliferative activity against HUVEC cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
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42593922 |
| BEAS-2B | IC50 |
96.71 μM
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Antiproliferative activity against BEAS-2B cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
Antiproliferative activity against BEAS-2B cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
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42593922 |
| HEK-293T | IC50 |
48.72 μM
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Antiproliferative activity against 293T cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
Antiproliferative activity against 293T cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
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42593922 |
| COS-7 | IC50 |
76.76 μM
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Antiproliferative activity against COS-7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
Antiproliferative activity against COS-7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay.
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42593922 |
In Vitro
ROCK2-IN-19, the non-isotopic form of compound 22d, potently and selectively inhibits purified ROCK2 with an IC50 of 13 nM, showing a selectivity of ≥769-fold over ROCK1. It also exhibits broad kinome selectivity, with its potent activity primarily restricted to ROCK2 and a small number of AGC family kinases[1].
ROCK2-IN-19 inhibits the proliferation of MDA-MB-231 human triple-negative breast cancer cells with an IC50 of 14.48 μM, and exhibits only weak antiproliferative activity against normal cell lines[1].
ROCK2-IN-19 (2.5-20 μM; 48 h) potently and concentration-dependently inhibits the migration of human triple-negative breast cancer cell line MDA-MB-231[1].
ROCK2-IN-19 (2.5-20 μM) dose-dependently inhibits ROCK2 activity and suppresses the phosphorylation of STAT3 at the Tyr705 site in human triple-negative breast cancer cell line MDA-MB-231[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 human triple-negative breast cancer cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Inhibited migration of MDA-MB-231 human triple-negative breast cancer cells in a concentration-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG mice (female, 6 weeks old, tail vein injection of 1 × 106 MDA-MB-231-luc cells)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 35 days
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Result:Significantly inhibited lung metastasis compared with vehicle control, with efficacy comparable to the positive control KD025.
Showed no significant body weight loss.
Chemical Information
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Molecular Weight 426.47
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Formula C25H22N4O3
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SMILES
O=C(N(C)C1=CC(C2=C3C(NC=C3)=NC=C2)=CC=C14)CN(CC5=CC=CC(OC)=C5)C4=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ROCK2-IN-19 Related Classifications
HY-189083 Related Classifications
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