TBOPP

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Chemical Structure| 1996629-79-8 同义名 : -
CAS号 : 1996629-79-8
货号 : A1216714
分子式 : C24H21F3N2O4S
纯度 : 99%+
分子量 : 490.495
MDL号 : MFCD32215320
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(214.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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 KD 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.39mL

4.08mL

2.04mL
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