2. Epigenetics PI3K/Akt/mTOR Cell Cycle/DNA Damage Stem Cell/Wnt
  3. AMPK MARK YAP
  4. 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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OICR19451

OICR19451 Chemical Structure

CAS No. : 2803349-61-1

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OICR19451 Related Antibodies

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

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Description

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[1].

IC50 & Target[1]

NUAK1

12 nM (IC50)

NUAK2

10 nM (IC50)

MARK2

101 nM (IC50)

MARK3

124 nM (IC50)

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.

OICR19451 Related Antibodies
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.
Molecular Weight

593.09

Formula

C26H31ClF2N8O2S
CAS No.
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
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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OICR19451 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:

OICR194512803349-61-1OICR 19451OICR-19451AMPKMARKYAPAMP-activated protein kinaseMicrotubule affinity regulating kinaseYes-associated proteinMARK2TAZNUAK1Caco-2NUAK2MDA-MB-231 cellsMARK3triple-negative breast cancerHippo pathwayInhibitorinhibitorinhibit

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