1. PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  2. PI3K Reactive Oxygen Species Apoptosis
  3. GO-203 TFA

GO-203 TFA 是一种有效的 MUC1-C 癌蛋白抑制剂。GO-203 TFA 是一种全 D 氨基酸肽,由与 CQCRRKN 基序连接的聚 R 转导结构域组成,该基序与 MUC1-C 胞质尾部结合并阻断 MUC1-C 同二聚化。GO-203 TFA 通过抑制 PI3K-AKT-S6K1 途径下调 TIGAR (TP53 诱导的糖酵解和凋亡调节剂) 蛋白合成。GO-203 TFA 诱导 ROS 的产生和线粒体跨膜电位的丧失。GO-203 TFA 可抑制体外结肠癌细胞和裸鼠异种移植物的生长。

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Custom Peptide Synthesis

GO-203 TFA Chemical Structure

GO-203 TFA Chemical Structure

CAS No. : 1222186-26-6

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MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice[1][2].

IC50 & Target[2]

PI3K

 

体外研究
(In Vitro)

GO-203 TFA (5 μM;三天) 通过降低细胞内 GSH 水平和增强 ROS 产生来抑制 MUC1 阳性结直肠癌细胞增殖。GO-203 TFA 对 MUC1 阴性 SW480 和 LOVO 细胞的细胞生长没有影响[2]
GO-203 (5 μM;三天) TFA 诱导 SKCO-1 细胞约 80% 死亡。GO-203 TFA 导致线粒体膜电位显着降低[2]
GO-203 (5 μM;持续三天) TFA 抑制结直肠癌细胞中的 AKT-mTORC-S6K1 翻译途径[2]
GO-203 (5 μM;持续三天) TFA 显着降低 SKCO-1 细胞中的 GSH 水平[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Inhibited MUC1 positive colorectal cancer cell proliferation.

Apoptosis Analysis[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Induced approximately 80% death and resulted in a significant decrease in mitochondrial membrane potential.

Western Blot Analysis[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Inhibited the activation of S6K1 in SKCO-1 cells.
Inhibited the degradation of PDCD4.
体内研究
(In Vivo)

GO-203 (18 mg/kg/天;腹腔注射;持续 28 天) TFA 显着抑制 COLO-205 肿瘤的生长[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four- to 6-week-old BALB/c nu/nu male/female mice with Colo-205 or SKCO-1 cells[2]
Dosage: 18 mg/kg
Administration: IP; daily; for 28 days
Result: Significantly inhibited growth of the COLO-205 tumors.
These tumors regressed completely by the end of treatment (day 28) and there was no evidence for regrowth by day 180.
分子量

2426.77

Formula

C89H171F3N52O21S2

CAS 号
性状

固体

颜色

White to off-white

Sequence

d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)

Sequence Shortening

d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (41.21 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 100 mg/mL (41.21 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4121 mL 2.0604 mL 4.1207 mL
5 mM 0.0824 mL 0.4121 mL 0.8241 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.28%

参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.4121 mL 2.0604 mL 4.1207 mL 10.3018 mL
5 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0604 mL
10 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0302 mL
15 mM 0.0275 mL 0.1374 mL 0.2747 mL 0.6868 mL
20 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5151 mL
25 mM 0.0165 mL 0.0824 mL 0.1648 mL 0.4121 mL
30 mM 0.0137 mL 0.0687 mL 0.1374 mL 0.3434 mL
40 mM 0.0103 mL 0.0515 mL 0.1030 mL 0.2575 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GO-203 TFA
目录号:
HY-P1925A
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