MALT1-IN-9 (WO2021000855A1, Compound 5), a highly potent inhibitor of MALT1 protease, demonstrates an IC50 value of <500 nM when tested in Raji MALT1-GloSensor cells. MALT1-IN-9 exhibits significant anticancer properties [1].
Irreversible MALT1 inhibitor. Suppresses T cell activation-induced cleavage of Bcl-10 in a dose-dependent manor. Reduces Jurkat cell adhesion to fibronectin. Cell permeable.
MLT-231, a potent and highly selective allosteric MALT1 inhibitor, has an IC50 of 9 nM and specifically inhibits endogenous BCL10 cleavage with an IC50 of 160 nM. It exhibits antitumor activity in an ABC-DLBCL type xenograft mouse model[1].