606968-52-9
Chemical Structure
FC131
- CAS No.: 606968-52-9
- Formula:C36H47N11O6
- Molecular Weight:729.83
IUPAC Name: 1,1'-(((2S,5S,8S,14R)-14-(4-hydroxybenzyl)-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecane-2,5-diyl)bis(propane-3,1-diyl))diguanidine
InChIKey: MBXBICVKLVYNKD-XFTNXAEASA-N
SMILES: O=C([C@@H](NC([C@@H](NC([C@@H](CC1=CC=C(O)C=C1)NC(CNC2=O)=O)=O)CCCNC(N)=N)=O)CCCNC(N)=N)N[C@H]2CC3=CC4=C(C=CC=C4)C=C3
Biological Activity: FC131 is a CXCR4 antagonist that inhibits AKT kinase activity in AML OCI-AML3 cells. D-ArgFC131, a derivative of FC131, inhibits the phosphorylation of downstream ERK1/2 and Akt, induces caspase-3 pathway-mediated apoptosis, and causes cell cycle arrest. FC131 exerts cytotoxic effects in cancer cells such as AML cells. FC131 is applicable for cancer-related research[1][2][3].
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FC131 | FC131 is a CXCR4 antagonist that inhibits AKT kinase activity in AML OCI-AML3 cells. D-ArgFC131, a derivative of FC131, inhibits the phosphorylation of downstream ERK1/2 and Akt, induces caspase-3 pathway-mediated apoptosis, and causes cell cycle arrest. FC131 exerts cytotoxic effects in cancer cells such as AML cells. FC131 is applicable for cancer-related research. | |||||||||||||||||||||
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- [1]. Mandawat A, et al. Pan-histone deacetylase inhibitor panobinostat depletes CXCR4 levels and signaling and exerts synergistic antimyeloid activity in combination with CXCR4 antagonists. Blood. 2010 Dec 09;116(24):5306-15. [Content Brief]
- [2]. Kim JM, et al. The cyclic pentapeptide d-Arg3FC131, a CXCR4 antagonist, induces apoptosis of somatotrope tumor and inhibits tumor growth in nude mice. Endocrinology. 2011 Feb;152(2):536-44. [Content Brief]
- [3]. Thiele S, et al. Determination of the binding mode for the cyclopentapeptide CXCR4 antagonist FC131 using a dual approach of ligand modifications and receptor mutagenesis. British journal of pharmacology. 2014 Dec;171(23):5313-29. [Content Brief]
Keywords
