1426227-11-3
Chemical Structure
D-CopA3
- CAS No.: 1426227-11-3
- Formula:C96H184N30O18S2
- Molecular Weight:2110.81
InChIKey: CLSVYAPBZHDADS-AKTRCOMQSA-N
SMILES: NCCCC[C@H](C(N)=O)NC([C@@H](CCCCN)NC([C@@H](CCCNC(N)=N)NC([C@@H](CC(C)C)NC([C@@H](C)NC([C@@H]([C@H](C)CC)NC([C@@H](CSSC[C@@H](NC([C@@H](CC(C)C)NC([C@H](N)CC(C)C)=O)=O)C(N[C@H]([C@H](C)CC)C(N[C@H](C)C(N[C@H](CC(C)C)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCCN)C(N[C@@H](C(N)=O)CCCCN)=O)=O)=O)=O)=O)=O)NC([C@@H](CC(C)C)NC([C@H](N)CC(C)C)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models[1][2].
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D-CopA3 | D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models. | |||||||||||||||||||||
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References
- [1]. Kim DH, et al., The Insect Peptide CopA3 Increases Colonic Epithelial Cell Proliferation and Mucosal Barrier Function to Prevent Inflammatory Responses in the Gut. J Biol Chem. 2016 Feb 12;291(7):3209-23. [Content Brief]
- [2]. Dey DK, et al., CopA3 peptide inhibits MDM2-p53 complex stability in colorectal cancers and activates p53 mediated cell death machinery. Life Sci. 2023 Apr 1;318:121476. [Content Brief]
