500272-80-0
Chemical Structure
CInQ-03
- CAS No.: 500272-80-0
- Formula:C22H12ClN5O
- Molecular Weight:397.82
IUPAC Name: 2-chloro-N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)benzamide
InChIKey: HLFGQICCFZTXTP-UHFFFAOYSA-N
SMILES: O=C(NC1=CC2=C(C#N)C3=NC4=CC=CC=C4N=C3N2C=C1)C5=CC=CC=C5Cl
Biological Activity: 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[1][2][3].
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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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References
- [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]
- [2]. Cheng Y. Design, Synthesis and Biological Evaluation of the Novel MEK Inhibitor and Radioprotectors [doctoral thesis]. Adelaide: Flinders University; 2021.
- [3]. Cheng Y, et al. Current Development Status of MEK Inhibitors. Molecules (Basel, Switzerland). 2017 Sep 26;22(10):1551. [Content Brief]
