TBOPP_product_DataBase

Bioactivity

TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors[1].

Target

IC50: 8.4 μM (DOCK1); Kd: 7.1 μM (DOCK1 DHR-2 domain)

Invitro

TBOPP (12.5 µM; 3 days; 3LL cells) treatment inhibits DOCK1-mediated invasion, macropinocytosis, and survival under the condition of glutamine deprivation without impairing the biological functions of the closely related DOCK2 and DOCK5 proteins[1]. Cell Viability Assay[1] Cell Line:

In Vivo

TBOPP (0.67 mg per mouse; administrated on days 0, 1, 3, and 5; for 2 weeks; C57BL/6 mice) treatment effectively suppresses metastasis of cancer cells in vivo and the number of lymphocytes in the spleen is not changed, the body weight is also unchanged between TBOPP-treated and non-treated mice[1]. Animal Model:

Name

TBOPP

CAS

1996629-79-8

Formula

C24H21F3N2O4S

Molar Mass

490.49

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. 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.

PeptideDB

TBOPP

CAS: 1996629-79-8 F: C24H21F3N2O4S W: 490.49