RGNCY-0059 (NUCC-390 CXCR4 agonist)

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NUCC-390 is a the first small molecule agonist of the CXCR4 receptor.  The CXCR4 receptor is involved in a large number of physiological processes including HIV infectivity, inflammation, tumorigenesis, stem cell migration and autoimmune disease. The agonist profile of NUCC-390 was determined through Ca imaging, ERK activation, receptor internalization and chemotaxis assays and was shown to be similar to the SDF-1 agonist.  Interestingly, NUCC-390 did not compete with SDF-1 for binding to the CXCR4 receptor suggesting that their sites of interaction are not identical.  The in vitro physiological effects of NUCC390 were inhibited by the selective CXCR4 antagonist AMD3100.  NUCC-390 provides an excellent and unique probe to further study the in function of the CXCR4 receptor. 

Systematic Name:  piperidin-1-yl(1-propyl-5-((2-(pyridin-4-yl)ethyl)amino)-4,5,6,7-tetrahydro-1H-indazol-3-yl)methanone


Formula:  C23H33N5O

Mol Wt:   395.55

PMID:  27456816

Tags: Cancer, ERK, stem cell, inflammation, Tumor, NUCC-390, CXCR4, HIV, autoimmune, SDF-1, AMD3100, RHNCY-0059