PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study.
PROTAC TG2 degrader-2 (Compound 7) (10 μΜ, up to 24h) inhibits the migration of OVCAR5 and SKOV3 cell lines in both wound-healing assays and transwell migration assays[1].PROTAC TG2 degrader-2 (10 μΜ) reduces the adhesion of OVCAR5 and SKOV3 cells to fibronectin[1].PROTAC TG2 degrader-2 (up to 10 μΜ, 6 h) reduces the level of Transglutaminase 2(TG2) within 6 h in a concentration-dependent manner in both OVCAR5 and SKOV3 cells[1].
References:
[1]. Valdivia A, el at. Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2). J Med Chem. 2023;66(14):9445-9465. doi:10.1021/acs.jmedchem.2c01859Valdivia A, Vagadia PP, Guo G, O'Brien E, Matei D, Schiltz GE. Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2). J Med Chem. 2023;66(14):9445-9465. doi:10.1021/acs.jmedchem.2c01859