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Art. -Nr.: HY-189083

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₅H₂₂N₄O₃
Molecular Weight:426.47

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ROCK2-IN-19 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

ROCK2

13 nM (IC₅₀)

STAT3

Alle ROCK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	14.48 μM	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.	42593922
HUVEC	IC50	51.19 μM	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.	42593922
BEAS-2B	IC50	96.71 μM	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.	42593922
HEK-293T	IC50	48.72 μM	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.	42593922
COS-7	IC50	76.76 μM	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.	42593922

In Vitro

OthersAnti-cancer

Others

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].

Anti-cancer

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.

Cell Migration Assay ^[1]

Cell Line:

MDA-MB-231 human triple-negative breast cancer cells
Concentration:

2.5, 5, 10 μM
Incubation Time:

48 h
Result:

Inhibited migration of MDA-MB-231 human triple-negative breast cancer cells in a concentration-dependent manner.

In Vivo

Anti-cancer

ROCK2-IN-19 (100 mg/kg; p.o.; once daily; for 35 days), the non-isotopic form of compound 22d, effectively inhibits lung metastasis of MDA-MB-231 breast cancer in female NCG mice with extremely low toxicity^[1].

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

Animal Model:

NCG mice (female, 6 weeks old, tail vein injection of 1 × 10⁶ MDA-MB-231-luc cells)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; daily; 35 days
Result:

Significantly inhibited lung metastasis compared with vehicle control, with efficacy comparable to the positive control KD025.
Showed no significant body weight loss.

Related Protocols :

Chemical Information

Molecular Weight 426.47
Formel C₂₅H₂₂N₄O₃
SMILES

O=C(N(C)C1=CC(C2=C3C(NC=C3)=NC=C2)=CC=C14)CN(CC5=CC=CC(OC)=C5)C4=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li Y, et al. Discovery of Deuterated 3,4-Dihydro-benzo[e][1,4]diazepine-2,5-dione Derivatives as Potent, Selective and Orally Bioavailable ROCK2 Inhibitors. J Med Chem. 2026 Aug 13;69(15):17854-17880.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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ROCK2-IN-19

Alle ROCK Isoform-spezifische Produkte anzeigen

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