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MALT1 inhibitor MI-2 (ABM-3912) binds directly to MALT1 and irreversibly suppresses protease function. MALT1 inhibitor MI-2 (ABM-3912) decreases NF-κB activity induced by MALT1. MALT1 inhibitor MI-2 (ABM-3912) inhibits cell proliferation and MALT1-mediated cleavage activity. MALT1 inhibitor MI-2 (ABM-3912) concentrates within human ABC-DLBCL cells and irreversibly inhibited cleavage of MALT1 substrates. MALT1 inhibitor MI-2 (ABM-3912) displayes selective activity against ABC-DLBCL cell lines in vitro and xenotransplanted ABC-DLBCL tumors in vivo.
| Cell Experiment | |
|---|---|
| Cell lines | MLL-AF9 and E2A-HLF transduced murine BMC |
| Preparation method | Plating the MLL-AF9 and E2A-HLF transduced murine BMC in 12-well plates at the concentration of 5×103 cells/mL with 1 mL methylcellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds.After 6 days staining colonies with 100 μL iodonitrotetrazolium chloride at final concentration of 1 mg/mL, incubating at 37°C for 30 min and counting . To replate for the 2nd round, counting colonies at day 6 without staining and washing cells out by 1×PBS buffer and resuspending in IMDM medium which contains 15% FBS, 1% penicillin/streptomycin and IL-3.Plateing 5×103 cells in 12-well plates with 1ml methycellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later staining and counting colonies . |
| Concentrations | ~20 μM |
| Incubation time | 12 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 455.72 |
| Formula | C19H17Cl3N4O3 |
| CAS Number | 1047953-91-2 |
| Solubility (25°C) | DMSO ≥ 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MALT1 Products |
|---|
| 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. |
| JNJ-67856633
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective mucosa-associated lymphoid tissue protein 1 (MALT1) allosteric inhibitor for studies related to chronic lymphocytic leukemia (CLL). |
| MLT-943
MLT-943 is a potent, selective, and orally active inhibitor of mucosa-associated lymphoid tissue protein 1 (MALT1) that inhibits IL-2 secretion in PBMC or whole blood with IC50 values of 0.07-0.09 μM and 0.6-0.8 μM, respectively.In addition, MLT-943 possesses anti-inflammatory activity and can be used in studies of FcgR-mediated inflammation . |
| SGR-1505
SGR-1505 is an oral potent small molecule allosteric inhibitor of MALT1 that inhibits MALT1 enzymatic activity and demonstrates anti-proliferative activity in ABC-DLBCL cell lines, both BTKi-sensitive (OCI-LY10) and BTKi-resistant (OCI-LY3). SGR-1505 can be used in studies related to B-cell tumors. |
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