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CAS No.: 1996629-79-8

TBOPP Catalog No. CSN27204

TBOPP is a selective DOCK1 inhibitor with IC50 value of 8.4μM. It dampened DOCK1-mediated invasion, macropinocytosis, and survival under the condition of glutamine deprivation. TBOPP treatment suppressed cancer metastasis and growth in vivo in mice.

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400-920-2911

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技术信息

生物活性

描述The dedicator of cytokinesis (DOCK) family is one of the two members of the RAC guanine nucleotide exchange factor (GEF) family. DOCK1 regulates phagocytosis, myoblastic fusion, cell migration and circular dorsal fold formation^[2]. TBOPP is a selective inhibitor of Dock1 which inhibits Dock1-mediated Rac activation with an IC₅₀ of 8.4 μM and binds DOCK1 DHR-2 domain with a K_D of 7.1 mM^[3]. TBOPP decreased RCC (renal cell carcinoma) cell viability from 10 µM in a concentration-dependent manner and significantly decreased cell proliferation at 10 and 40 µM. TBOPP (10 µM) inhibited RCC cell cisplatin resistance in RCC cells^[2]. TBOPP treatment for 48 hr induced a significantly high level of cell death in JEG-3 cells^[4].
作用机制TBOPP binds to the DHR-2 domain of DOCK1^[2].
参考文献

[1] Tajiri H, Uruno T, Shirai T, et al. Targeting Ras-Driven Cancer Cell Survival and Invasion through Selective Inhibition of DOCK1. Cell Rep. 2017;19(5):969-980. doi:10.1016/j.celrep.2017.04.016
[2] Zhang W, et al. TBOPP enhances the anticancer effect of cisplatin by inhibiting DOCK1 in renal cell carcinoma. Mol Med Rep. 2020 Aug;22(2):1187-1194
[3] Tajiri H, et al. Targeting Ras-Driven Cancer Cell Survival and Invasion through Selective Inhibition of DOCK1. Cell Rep. 2017 May 2;19(5):969-980
[4] Franklin GA, et al. Decreased juvenile arson and firesetting recidivism after implementation of a multidisciplinary prevention program. J Trauma. 2002 Aug;53(2):260-4; discussion 264-6

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0388 mL
- 10.1938 mL
- 20.3876 mL
- 5 mM
- 0.4078 mL
- 2.0388 mL
- 4.0775 mL
- 10 mM
- 0.2039 mL
- 1.0194 mL
- 2.0388 mL

技术信息

CAS号

1996629-79-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H21F3N2O4S

运输

蓝冰

分子量

490.49

别名

溶解度

DMSO	97.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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