tg2

ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease.

TG2-IN-3h is a transglutaminase (TGase) inhibitor used in the study of neurological and immune system disorders.

AA10 is an irreversible inhibitor of transglutaminase 2 (TG2).

NC9 is an irreversible inhibitor of transglutaminase 2 (TG2) and also inhibits Factor XIIIA (FXIIIA).

VA5 is an transamidase inhibitor by direct binding at the transamidase site. VA5 also inhibits GTP-binding activities. It interaction at the transamidase site locks the protein in the extended/open conformation to disorganize/inactivate the GTP binding/GT

AA9 is a novel transglutaminase (TG2) inhibitor.

VA4 is a novel irreversible TG2 transamidase site-specific inhibitor.

PROTAC TG2 degrader-2 (compound 7) is a selective competitive degrader of Transglutaminase 2 (TG2) with a dissociation constant (Kd) greater than 100 μM. It inhibits cell migration and reduces TG2 levels in ovarian cancer cells, making it a valuable tool for ovarian cancer research [1].

PROTAC TG2 Degrader-1 (Compound 11) is a VHL-based PROTAC that targets tissue transglutaminase (TG2) and exhibits a binding affinity with a K D of 68.9 μM. This compound effectively decreases TG2 levels in ovarian cancer cells through a proteasome-dependent pathway [1].

TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity. TG2-179-1 exhibits potent cytotoxic activity against colon cancer cells and induces apoptosis. TG2-179-1 can be used in colon cancer research. TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity.

MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.

TG53 is a tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction inhibitor.

BJJF078, an aminopiperidine derivative, is a potent inhibitor of recombinant human and mouse glutamine aminotransferase (TG2) activity, with IC50 values of 41 and 54 nM for human and mouse glutamine aminotransferase, respectively.BJJF078 inhibits TG1 enzyme, with an IC50 of 0.16 μM.BJJF078 can be used to study multiple sclerosis (MS). BJJF078 can be used to study multiple sclerosis (MS).

PNU-145156E free base is an angiogenesis inhibitor.

CP4d is a novel reversible tg2 transamidase site-specific inhibitor

Zampilimab (UCB-7858), a monoclonal antibody targeting transglutaminase 2 (TG2), exhibits potential applications in renal transplantation [1] [2].

MD102, with an IC50 value of 0.35 μM, is a potent TG2 inhibitor that stabilizes p53 by inhibiting TG2. This results in a decrease in p-AKT and p-mTOR downstream signaling, ultimately inducing tumor cell apoptosis [1].

TG-2-IN-4 (compound 8), an inhibitor of transglutaminase 2 (TG2) with an IC 50 value of less than 0.5 mM, is utilized in the study of inflammatory disorders [1].

HB-3-20 induces the degradation of integrin αVβ5 on the cell surface. Transglutaminase 2 (TG2) specifically interacts with HB-3-20, exhibiting a catalytic efficiency (kcat KM) of 0.16 μM^-1min^-1.