Stauprimide

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Stauprimide 

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

Stauprimide Chemical Structure

CAS No. : 154589-96-5

规格 是否有货
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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

Cell Line: Renal cancer cell line RXF 393 cells and CAKI-1 cells
Concentration: 5 μM
Incubation Time: 3 hours
Result: Decreased nuclear localized NME2.

RT-PCR[1]

Cell Line: CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells
Concentration: 4μM, 6μM, 8μM, 10μM
Incubation Time: 6 hours
Result: 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
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice[1]
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.

分子量

584.62

Formula

C35H28N4O5

CAS 号

154589-96-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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

参考文献
  • [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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Cas(154589-96-5), Stauprimide, ,Stauprimide,

Stauprimide,抑制剂

抑制NME2核易位;灌注ESC以分化
99%

有货

Cas(154589-96-5), Stauprimide, ,Stauprimide,

CAS编号 154589-96-5 | 品牌:Jinpan
Stauprimide

MSDS

质检证书(CoA)

相似产品

  • 分子式 C35H28N4O5
  • 分子量584.62
  • PubChem编号 46245328

货号 (SKU) 包装规格 是否现货 价格 数量
S139814-1mg 1mg 现货 Cas(154589-96-5), Stauprimide, ,Stauprimide,  
S139814-5mg 5mg 现货 Cas(154589-96-5), Stauprimide, ,Stauprimide,  

基本信息

产品名称 Stauprimide,抑制剂
英文名称 Stauprimide
别名 N-Benzoyl-7-oxostaurosporine
英文别名 N-Benzoyl-7-oxostaurosporine
规格或纯度 99%
运输条件 超低温冰袋运输
生化机理 引发胚胎干细胞(ESC)分化的小分子。与NME2相互作用并抑制其核易位。提高小鼠和人ESCs体外定向分化的效率。

一般描述

Stauprimide is an indolocarbazole semi-synthetic small molecule shown to significantly increase the efficiency of directed embryonic stem cell differentiation. Stauprimide inhibits the nuclear localization of NME2, blocking and downregulating c-Myc expression. The expression of c-Myc is crucial for embryonic stem cell self-renewal, and intervention by Stauprimide allows for more efficient lineage-specific differentiation. NME2 is also indicated to be upregulated in certain cancers, indicating further application for the blocking action of StauprimideAn indolocarbazole promoter of embryonic stem cell differentiation.

Stauprimide is an indolocarbazole semi-synthetic small molecule shown to significantly increase the efficiency of directed embryonic stem cell differentiation. Stauprimide inhibits the nuclear localization of NME2, blocking and downregulating c-Myc expression. The expression of c-Myc is crucial for embryonic stem cell self-renewal, and intervention by Stauprimide allows for more efficient lineage-specific differentiation. NME2 is also indicated to be upregulated in certain cancers, indicating further application for the blocking action of Stauprimide
An indolocarbazole promoter of embryonic stem cell differentiation.

相关属性

CAS编号 154589-96-5
敏感性 对光敏感
熔点 145°C
溶解性 Soluble in DMSO}
储存温度 -20°C储存
分子量 584.62
分子式 C35H28N4O5
品牌 Jinpan
PubChem CID 46245328