Stauprimide (Synonyms: NBenzoyl7oxo Staurosporine) |
Catalog No.GC17839 |
La estauprimida es un anÁlogo de estaurosporina que promueve la diferenciaciÓn de células madre embrionarias (ESC). La estauprimida es un inhibidor de espectro no amplio que se une al factor de transcripciÓn NME2 de MYC y bloquea su localizaciÓn nuclear en las ESC, lo que da como resultado una regulaciÓn negativa de la transcripciÓn de MYC.
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Cas No.: 154589-96-5
Sample solution is provided at 25 µL, 10mM.
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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