Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which causes down-regulation of MYC transcription.

Stauprimide (10 μM; 6 hours) inhibits MYC transcription in the majority of cell lines tested (EC50: range of 30 nM-8 μM). It also decreases MYC levels between 15% to over 90%. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro (IC50: 780 nM in RXF 393 cells). Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines [1].

Stauprimide (p.o.; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, decreases MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells. It also inhibits MYC transcription in the RXF 393 tumor [1].