Transglutaminase Inhibitor

WRR139 is a peptide vinyl sulfone involving in disease processes such as inflammation and cancer. WRR139 is also a cytosolic enzyme N-glycanase 1 (NGLY1) and Nrf1 inhibitor. WRR139 enhances Carfilzomib cytotoxicity against cancer cells.

MT-4 is a derivative of a tissue transglutaminase (TG2) inhibitor. MT-4 targets the complex of TG2 and fibronectin (FN) (TG2/FN) and inhibits the adhesion of tumor cells to the matrix. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum and increases the sensitivity of OC cells to paclitaxel.

Suvigletistat is a Transglutaminase 2 (TG2) inhibitor with an IC₅₀ <0.5 μM. Suvigletistat can be used for the research of inflammatory disorders.

HB-230 is a Transglutaminase-2 (TG2) (human IC₅₀ = 4.9 μM) inhibitor and a selective fluorescent imaging probe for active TG2 localization. HB-230 modifies TG2 Cys277 to sustain the enzyme open conformation. HB-230 forms a ternary complex with TG2 and α2-macroglobulin, undergoes receptor-mediated endocytosis, and trafficks directly to lysosomes without early/late endosome fusion. HB-230 exhibits TG2 activity-dependent and α2-macroglobulin-dependent uptake. HB-230 can be used for the research of celiac disease, (Ex/Em = 649/665 nm).

PROTAC TG2 Degrader-3 is a TG2 (TGM2) PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer.