MALT1 inhibitor (ABM-3912) binds directly to MALT1 and irreversibly suppresses protease function. MALT1 inhibitor (ABM-3912) decreases NF-κB activity induced by MALT1. MALT1 inhibitor (ABM-3912) inhibits cell proliferation and MALT1-mediated cleavage activity. MALT1 inhibitor (ABM-3912) concentrates within human ABC-DLBCL cells and irreversibly inhibited cleavage of MALT1 substrates. MALT1 inhibitor (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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related MALT1 Products |
|---|
| Val-Arg-Pro-DL-Arg-Fluoromethylketone
Val-Arg-Pro-DL-Arg-Fluoromethylketone is a potent MALT1 inhibitor. |
| Mepazine
Mepazine is a potent and selective inhibitor of MALT1 protease, with IC50s of 0.83 and 0.42 μM for inhibition of full-length GSTMALT1 and GSTMALT1 325-760 segments, respectively, and also affects the viability of ABC-DLBCL cells by enhancing apoptosis. Mepazine also affects the viability of ABC-DLBCL cells by enhancing apoptosis. |
| MPT-0118
MPT-0118 is an S-enantiomer of methylpiperazine and a MALT1 inhibitor that can be used in studies related to B-cell tumors. |
| 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. |
| ABBV-525
ABBV-525 is a MALT1 inhibitor for studies related to B-cell chronic lymphocytic leukemia, diffuse large B-cell lymphoma. |
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