RGT-068A is a potent, selective and oral bioavailable MALT1 inhibitor[1].
JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis[1][2][3].
Val-Arg-Pro-DL-Arg-Fluoromethylketone is a potent MALT1 inhibitor. Val-Arg-Pro-DL-Arg-Fluoromethylketone inhibits cell proliferation and migration. Val-Arg-Pro-DL-Arg-Fluoromethylketone shows anticancer activity[1].
MI 2 (MALT1 inhibitor) is an irreversible MALT1 protease inhibitor with an IC50 of 5.84 μM.
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis[1].
MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research[1].
(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research[1].
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression[1].
(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].
MALT1-IN-3 (compound 122) is a potent MALT1 protease inhibitor, with an IC50 of 0.06 μM. MALT1-IN-3 has IC50 of 0.14 and 0.13 μM for human IL6/IL10 in OCI-LY3 cells, respectively[1].
MALT1-IN-9 is a potent MALT1 protease inhibitor with a IC50 of <500 nM in Raji MALT1-GloSensor cells. MALT1-IN-9 has anticancer effects (WO2021000855A1; Compound 5)[1].
MLT-748 is an allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM. MLT-748 also reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM)[1].
(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1)[1].
MALT1-IN-6 is a potent MALT1 protease inhibitor with a Ki of 9 nM. MALT1-IN-6 has anticancer effects (WO2018226150A1; Compound 4)[1].
(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC50 of 3 nM. (R)-MLT-985 has an IC50 of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells[1].
MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.
MLT-748 is a allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM. MLT-748 also reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM)[1].
MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research[1].
MALT1-IN-8 is a potent MALT1 protease inhibitor with a IC50 of 2 nM. MALT1-IN-8 inhibits the growth of OCI-LY3 lymphoma cells with an IC50 of 1.16 μM. MALT1-IN-8 has anticancer effects (WO2018165385A1; Compound 8)[1].
MALT1-IN-11 (Example 151 in reference Patent) is a MALT1 protease inhibitor (IC50 < 10 nM). MALT1-IN-11 inhibits IL10 secretion with an IC50 of 10-100 nM. MALT1-IN-11 can be used for the research of cancer, autoimmune and inflammatory disorders[1].
Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].