TTGM 5826

TTGM 5826 is a tissue transglutaminase (tTG) inhibitor with an EC₅₀ of 20 μM. TTGM 5826 stabilizes the open conformation of tTG that exhibits protein cross-linking activity, and acts as a competitive inhibitor of tTG-mediated cross-linking activity. TTGM 5826 inhibits the transformed phenotypes of breast cancer cells, brain cancer cells and glioma stem cells. TTGM 5826 can be used in the research of breast cancer, glioblastoma, pancreatic cancer and glioma stem cell-related tumors^[1]. In Vitro:TTGM 5826 (30 μM; 6 days) potently inhibits the growth of onco-Dbl-transformed MEF cells, while exerting minimal effects on untransformed MEF cells^[1].
TTGM 5826 (6 days) inhibits the growth of tTG-expressing cancer cell lines and GSCs, with IC₅₀ values ranging from 11 μM (GSC267) to 30 μM (Mia-PaCa-2, U-87 MG); it shows no effect on tTG-negative T47D and HME-1 cells, and exhibits enhanced activity against T98G cells with retinoic acid (HY-14649)-induced tTG upregulation^[1].
TTGM 5826 (15 μM; 12-36 h) significantly inhibits the migration of MDA-MB-231, U-87 MG and LN229 cancer cells^[1].
TTGM 5826 (15-30 μM; 10 days) completely blocks colony formation of MDA-MB-231 cells and potently inhibits colony formation of LN229 cells^[1].
TTGM 5826 (30-120 μM; 14 days) inhibits the anchorage-independent growth of LN229 and U-87 MG glioblastoma cells in a dose-dependent manner, with an inhibition rate of approximately 80%-85% at concentrations of 60-120 μM^[1].
TTGM 5826 (6.3-50.0 μM; 3 days) inhibits sphere formation (a marker of stem cell properties) in GSC374 and GSC267 glioma stem cells in a dose-dependent manner, and almost completely abolishes sphere formation at 50 μM^[1].