CInQ-03
CInQ-03 is an allosteric inhibitor of MEK1/2, with IC50 values of 5 μM and 10 μM against MEK1 and MEK2, respectively. CInQ-03 inhibits the kinase activity of MEK1/2 and reduces the phosphorylation levels of downstream ERK1/2 and RSK. CInQ-03 suppresses both anchorage-dependent and anchorage-independent growth of colon cancer cells, the activity of AP-1 reporter gene in colon cancer cells, as well as EGF-induced growth, transformation and AP-1 reporter gene activity in HaCaT keratinocytes. CInQ-03 can be used in studies related to colon cancer.
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- CAS No.: 500272-80-0
- Formule: C22H12ClN5O
- Masse moléculaire:397.82
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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MEK1 5 μM (IC50) |
MEK2 10 μM (IC50) |
erk1 |
ERK2 |
RSK |
CInQ-03 (5-10 μM; 2 h pre-incubation, then 12-24 h EGF stimulation) suppresses EGF-induced AP-1 promoter activity in HaCaT human keratinocytes in vitro in a dose-dependent manner, with 10 μM causing stronger inhibition than 5 μM for both 12 h 10 ng/mL EGF and 24 h 20 ng/mL EGF stimulation[1].
CInQ-03 reduces ERK phosphorylation in cultured cells, confirming its target engagement in a cellular context[2].
CInQ-03 inhibits MEK1 (IC50 = 5 μM) and MEK2 (IC50 = 10 μM) kinases in vitro, with a binding mode consistent with established MEK inhibitors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cr:NIH(S), NIH Swiss nude (6-9 weeks old)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:i.p.; three times per week; 11 days
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Result:Suppressed HCT116 tumor growth by over 70% relative to vehicle-treated controls (P < 0.05).
Markedly decreased Ki-67 expression in tumor tissues, while Ki-67 expression in skin tissues was similar to vehicle-treated controls.
Strongly suppressed phosphorylated ERKs and phosphorylated RSK in tumor tissues.
Showed no overt signs of toxicity or significant body weight loss compared to the vehicle group.
Chemical Information
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CAS No. 500272-80-0
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Masse moléculaire 397.82
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Formule C22H12ClN5O
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SMILES
O=C(NC1=CC2=C(C#N)C3=NC4=CC=CC=C4N=C3N2C=C1)C5=CC=CC=C5Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kim DJ, et al. CInQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo. Carcinogenesis. 2013 May;34(5):1134-43. [Content Brief]
[3]. Cheng Y, et al. Current Development Status of MEK Inhibitors. Molecules (Basel, Switzerland). 2017 Sep 26;22(10):1551. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CInQ-03 Related Classifications
HY-130453 Related Classifications
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