malt

MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor.

MALT1-IN-14 (comp 2) is a potent and selective MALT1 inhibitor with an IC50 value of 0.081 μM, widely utilized in immunology and oncology research to suppress MALT1 protease activity, dissect NF-κB signaling cascades, and evaluate therapeutic approaches targeting lymphoid malignancies and inflammatory diseases driven by dysregulated immune activation.

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].

(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease, capable of inhibiting MALT1 activity and potentially mitigating the enhancement of MALT1 activity due to abnormal T-cell or B-cell receptor signaling, cancer, or inflammatory diseases. It has potential for studies related to MALT1-related diseases.

MALT1-IN-5 is a potent inhibitor of the MALT1 protease and can be used in cancer research.

MALT1-IN-8 is a potent inhibitor of MALT1 protease (IC50: 2 nM) that inhibits the growth of OCI-LY3 lymphoma cells (IC50: 1.16 μM) and exhibits anticancer activity.

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM, and demonstrates IC50 values of 60 nM and 40 nM for human IL6 and IL10, respectively, in OCI-LY3 cells.

MALT1-IN-3 is a potent inhibitor of MALT1 protease (IC50: 0.06 μM) with IC50 values of 0.14 and 0.13 μM for human IL6 and IL10, respectively, in OCI-LY3 cells.

(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor with potential applications in cancer research.

MALT1-IN-7 [compound 142b] is a potent MALT1 protease inhibitor with potential applications in cancer research.

MALT1-IN-6 is a MALT1 protease inhibitor (Ki: 9 nM) that exhibits anticancer activity.

MALT1-IN-11, a potent MALT1 protease inhibitor (IC 50 < 10 nM), effectively reduces IL10 secretion, exhibiting an IC 50 between 10-100 nM. This compound is primarily utilized in the study of cancer, autoimmune, and inflammatory disorders.

NVS-MALT1 is an allosteric inhibitor of MALT1 [1].

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

Ocipumaltib (Example 2) is an inhibitor of mucosa-associated lymphoid tissue protein 1 (MALT1). It functions as an antineoplastic agent and is utilized in the study of cancer, infections, neurological disorders, and hematological diseases.

MALT1-IN-13 (compound 10m) is an inhibitor of the mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1), forming a covalent and irreversible bond with the MALT1 protease, thereby inhibiting its activity with an IC50 of 1.7 μM. It suppresses the proliferation of ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1 cells. Additionally, MALT1-IN-13 regulates the mTOR and PI3K-Akt pathways.

Mepazine (Pecazine) is a potent and selective inhibitor of MALT1, inhibiting GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 μM and 0.42 μM, respectively. Mepazine enhances apoptosis and impacts cell viability.

MIR96-IN-1 selectively inhibits biogenesis of microRNA-96, upregulating a protein target (FOXO1) and inducing apoptosis in cancer cells.

MLT-747 is an effective and allosteric inhibitor of MALT1. It binds MALT1 in the allosteric Trp580 pocket (IC50: 14 nM).

MLT-748 is a MALT1 allosteric inhibitor that inhibits the growth of lung cancer cells. MLT-748 acts by blocking the protein hydrolyzing activity of MALT1.

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric inhibitor of MALT1 protease . JNJ-67856633 lead to tumor stasis in some cases.

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].

MLT-985, a highly selective allosteric MALT1 inhibitor, exhibits an IC50 value of 3 nM.

Mepazine hydrochloride (Pecazine hydrochloride) is a potent MALT1 inhibitor with anticancer and antitumor activities. Mepazine hydrochloride inhibits RANK-induced osteoclastogenesis, suppresses MALT1 activity and tumor growth in pancreatic cancer.