Stauprimide is a small molecule that increases the efficiency of mouse and human embryonic stem cell differentiation in conjunction with lineage specification cues (EC = 0.3 μM). It specifically inhibits the nuclear localization of NME2, which results in the suppression of c-Myc, a key regulator of pluripotency.
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.
体外研究
Staupriide (10 μM; 6 Hours) inhibits MYC transcription in most cell lines, with EC50 ranging from 30 nM to 8 μM, and reduces MYC levels by 15% to over 90%.
Staupriide (2-8 μM; 24-72 hours) downregulates MYC leading to in vitro cell proliferation inhibition, with an IC50 of 780 nM in RXF 393 cells.
Staupriide (5 μM; 3 hours) inhibits MYC transcription by reducing NME2 nuclear translocation.
Cell Proliferation Assay
Cell Line:
Renal cancer cell line RXF 393 cells
Concentration:
2 μM, 4 μM, 8 μM
Incubation Time:
24 hours, 48 hours, 72 hours
Result:
Inhibited cell proliferation at concentrations of 2-8 μM.
Western Blot Analysis
Cell Line:
Renal cancer cell line RXF 393 cells and CAKI-1 cells
Suppressed MYC transcription in KG1A cells with an EC50 of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide.
体内研究
Staupriide (oral administration; 50 mg/kg; Once a day; 30 days, 55 days) to block tumor growth, reduce MYC protein levels in RXF 393 or CAKI-1 cell xenograft mice, and inhibit MYC transcription in RXF 393 tumors.
Animal Model:
Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:
50 mg/kg
Administration:
Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:
Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.
分子式
C35H28N4O5
分子量
584.62
CAS号
154589-96-5
中文名称
抑胃酶氨酰u丙基亚胺
运输条件
Room temperature in continental US; may vary elsewhere.