Stauprimide (Synonyms:顺式1-苄基-4-甲基-3-甲氨基-哌啶盐酸盐;抑胃酶氨酰u丙基亚胺)
目录号 : KCM11651 CAS No. : 154589-96-5 纯度 : ≥98%
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.
规格 价格 是否有货 数量
500μg
In-stock
1mg
In-stock
5mg
In-stock

Other Forms of Rapamycin:

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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.

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
Concentration: 5 μM
Incubation Time: 3 hours
Result: Decreased nuclear localized NME2.

RT-PCR

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

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.

储存方式

-20°C, stored under nitrogen

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

溶解性数据
In Vitro: 

DMSO: 10 mg/mL (17.11 mM; Need ultrasonic and warming)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL
10 mM 0.1711 mL 0.8553 mL 1.7105 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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