For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I017871 |
| CAS Number | 1996629-79-8 |
| Synonyms | 1-[2-oxo-2-[4-[3-(trifluoromethyl)phenyl]phenyl]ethyl]-5-pyrrolidin-1-ylsulfonylpyridin-2-one |
| Molecular Formula | C24H21F3N2O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C24H21F3N2O4S/c25-24(26,27)20-5-3-4-19(14-20)17-6-8-18(9-7-17)22(30)16-28-15-21(10-11-23(28)31)34(32,33)29-12-1-2-13-29/h3-11,14-15H,1-2,12-13,16H2 |
| InChIKey | ZMPDEBWNVHAKBB-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)S(=O)(=O)C2=CN(C(=O)C=C2)CC(=O)C3=CC=C(C=C3)C4=CC(=CC=C4)C(F)(F)F |
| 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. |
