MALT1
MALT1 is a paracaspase, which is related to the caspase (cysteine-aspartic proteases) family of proteases but cleaves after Arg residues instead of Asp. MALT1 cleavage activity is linked to the pathogenesis of activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL), a chemoresistant form of DLBCL. MALT1 is a unique paracaspase protein that transduces aberrant oncogenic signaling in ABC-DLBCL. MALT1 represents a potentially important therapeutic target for ABC-DLBCL and MALT lymphoma. MALT1 small molecule inhibitors might be useful chemical tools for studying MALT1 biology and treating MALT1-addicted tumors.
Targets for MALT1
Products for MALT1
- Cat.No. Product Name Information
- GC62115 JNJ-67856633 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.
- GC36534 MALT1 inhibitor MI-2 A MALT1 inhibitor
- GC68218 Mepazine
- GC61041 Mepazine hydrochloride 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.
- GC62611 MLT-231 MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
- GC67992 MLT-747
- GC65301 MLT-748 MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM.
- GC62464 MLT-943 MLT-943 is a potent, selective and orally active MALT1 protease inhibitor.
- GC65505 MLT-985 MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.
- GC45192 Z-VRPR-FMK (trifluoroacetate salt) Z-VRPR-FMK is a selective, irreversible inhibitor of the paracaspase mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), an endopeptidase that targets BCL10 and reduces NF-κB activation in lymphocytes at 12.5 to 75 μM.