626252-75-3
Chemical Structure
CKD-712
- CAS No.: 626252-75-3
- Formula:C20H19NO2
- Molecular Weight:305.37
IUPAC Name: (S)-1-(naphthalen-1-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol
InChIKey: YGCQFKVNIBDJFW-SFHVURJKSA-N
SMILES: OC1=CC2=C([C@H](CC3=C(C=CC=C4)C4=CC=C3)NCC2)C=C1O
Biological Activity: CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway[2]. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway[1][2]. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells[1][2]. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer[1][2][3].
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CKD-712 | CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer. | |||||||||||||||||||||
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References
- [1]. Park JH, et al. Effects of the anti-sepsis drug, (S)-1-(α-naphthylmethyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (CKD-712), on mortality, inflammation, and organ injuries in rodent sepsis models. Arch Pharm Res. 2011 Mar;34(3):485-94. [Content Brief]
- [2]. Lee WS, et al. Synthesized tetrahydroisoquinoline alkaloid exerts anticancer effects at least in part by suppressing NF-κB-regulated proteins in A549 human lung cancer cells. Oncol Rep. 2015;33(3):1141-1146. [Content Brief]
- [3]. Chae JW, et al. Development of a LC-MS/MS method for the determination of CKD-712 in rat plasma: Application to a pharmacokinetic study in rats. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1061-1062:123-127. [Content Brief]
