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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 500272-80-0
- 分子式: C22H12ClN5O
- 分子量:397.82
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MEK アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 500272-80-0
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分子量 397.82
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CInQ-03 関連分類
HY-130453 関連分類
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