Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription^[1]. In Vitro: Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC₅₀ range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%^[1].
Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC₅₀ of 780 nM in RXF 393 cells^[1].
Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation^[1].
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].
In Vivo: Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor^[1].