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Art. -Nr.: HY-182743

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OICR19451

OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC₅₀ values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer.

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CAS. Nr.: 2803349-61-1
Formel: C₂₆H₃₁ClF₂N₈O₂S
Molecular Weight:593.09

Speicherung:

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

OICR19451 Chemical Structure

CAS. Nr.: 2803349-61-1

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

NUAK1

12 nM (IC₅₀)

NUAK2

10 nM (IC₅₀)

MARK2

101 nM (IC₅₀)

MARK3

124 nM (IC₅₀)

Alle AMPK Isoform-spezifische Produkte anzeigen :

Alle YAP Isoform-spezifische Produkte anzeigen :

In Vitro

OICR19451 modulates Hippo pathway activity in MDA-MB-231 cells, increasing YAP phosphorylation (EC₅₀ = 125 nM), driving cytoplasmic YAP/TAZ localization (EC₅₀ = 144 nM), and inhibiting cell growth (EC₅₀ = 202 nM)^[1].

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

In Vivo

OICR19451 (30-60 mg/kg; p.o.; daily; 14 days) inhibits tumor growth, reduces metastasis, decreases tumor YAP/TAZ levels, and prolongs survival in an orthotopic metastatic breast cancer mouse model^[1].

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

Animal Model:

NOD/SCID-gamma (NSG) (female, 10 weeks old)^[1]
Dosage:

30 mg/kg; 60 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Inhibited tumor growth relative to controls.
Prolonged survival relative to controls.
Reduced metastasis to peritoneal space (mesentery) and liver relative to controls.
Decreased YAP/TAZ protein levels in tumors (60 mg/kg group).
Induced widespread tumor necrosis and collagenous tumor encapsulation.
Caused acceptable, reversible body weight loss with no gross behavioral or CNS-related side effects.

Chemical Information

CAS. Nr. 2803349-61-1
Molecular Weight 593.09
Formel C₂₆H₃₁ClF₂N₈O₂S
SMILES

CN1CCN(CC1)C2CCN(CC2)C3=CC(OC(F)F)=C(C=C3)NC4=NC=C(C(NC5=C(SC=C5)C(N)=O)=N4)Cl
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]. Smil D, et al. Discovery and development of potent and selective dual NUAK/MARK inhibitors as Hippo pathway modulators for the treatment of cancer. Eur J Med Chem. Published online March 31, 2026. [Content Brief]

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.

Keywords

100 mg

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

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OICR19451

Alle AMPK Isoform-spezifische Produkte anzeigen

Alle YAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

OICR19451 Related Classifications

HY-182743 Related Classifications