Stauprimide (Synonyms: NBenzoyl7oxo Staurosporine) |
| Catalog No.GC17839 |
Stauprimide는 배아줄기세포(ESC) 분화를 촉진하는 스타우로스포린 유사체입니다. Stauprimide는 MYC 전사 인자 NME2에 결합하고 ESC에서 핵 국소화를 차단하여 MYC 전사의 하향 조절을 초래하는 비광역 스펙트럼 억제제입니다.
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Cas No.: 154589-96-5
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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].
References:
[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.
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