Stauprimide 是一种促进胚胎干细胞 (ESC) 分化的星形孢菌素类似物。Stauprimide 与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位，导致 MYC 转录的下调, 是一种非广谱抑制剂。

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.

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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%.
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.
Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation.
Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines.
has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal M

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-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Bouvard C, et al. Small molecule selectively suppresses MYC transcription in cancer cells. Proc Natl Acad Sci USA. 2017 Mar 28;114(13):3497-3502.