RGNCY-0064 (NASTRp (CREB)-CREB CBP inhibitor)

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NASTRp (Ntpthol AS-TR phosphate) is an inhibitor of cyclic-AMP responsive element-binding protein (CREB)-CREB binding protein (CBP) transcription factor complex.  NASTRp is a potential therapeutic agent for lung adenocarcinoma.  NASTRp was shown to inhibit oncogenic cell properties through cell cycle arrest with concomitant suppression of tumor-promoting autophagy with down-regulation of of Atg5-12 and Atg7 and accumulation of p62 in human lung cancer cell lines. Furthermore, NASTRp was also shown to induce expression of endoplasmic reticulum stress marker,s DDIT3/CHOP and led to apoptosis along with BIM induction.  NASTRp targeting the CREB-CBP transcription complex is a novel and potent anti-cancer agent showing multiple effects on critical pathways in cell biology.  This represents a novel class of targeted therapies in cancer.

Systematic Name:  3-((4-chloro-2-methylphenyl)carbamoyl)naphthalen-2-yl dihydrogen phosphate   


Formula:  C18H15ClNO5P

Mol Wt:  391.74

PMID:  25897662

Tags: Cancer, autophagy, small molecule, Tumor, NASTRp, RGNCY-0064, CREB, CBP, CREB binding protein, lung, adenocarcinoma, Atg, p62, DDIT3, CHOP