Home Immunology & Inflammation MALT inhibitor MLT-748 For research use only.

MLT-748

MLT-748 is a potent, selective and allosteric inhibitor of MALT1 with IC50 of 5 nM, binding at the interface between the caspase and immunoglobulin (Ig3) domains by displacing Trp580 and locking the catalytic site in an inactive state.

MLT-748 Chemical Structure

MLT-748 Chemical Structure

CAS: 1832578-30-9

Purity & Quality Control

Batch: S889801 DMSO] 98 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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Choose Selective MALT Inhibitors

Biological Activity

Description MLT-748 is a potent, selective and allosteric inhibitor of MALT1 with IC50 of 5 nM, binding at the interface between the caspase and immunoglobulin (Ig3) domains by displacing Trp580 and locking the catalytic site in an inactive state.
Targets
MALT1 [1]
(Cell-free assay)
5 nM
In vitro
In vitro

MLT-748 binds MALT1 in the allosteric Trp580 pocket. MLT-748 binds and stabilizes mutant MALT1-W580S. Cleavage of MALT1 substrates is blocked by MLT-748 in B and T cells. MLT-748 rescues MALT1 function in patient MALT1mut/mut lymphocytes.[1]
Cell Research Cell lines Immortalized B cells, human PBMCs, primary human CD3+ T cells, primary CD4+ lymphocytes
Concentrations 2 μM
Incubation Time 24 h
Method

To study MALT1-W580S function in downstream signaling after allosteric inhibitor stabilization, patient and unaffected donor B cells are pretreated with 2 μM MLT-748 for 24 h followed by 50 ng/mL PMA and 1 μM ionomycin stimulation for up to 1 h. For compound washout experiments, after 24-h pre-treatment of B cells with 2 μM MLT-748, the cells are washed in PBS three times, rested for 2-h compound free and then stimulated with PMA/ionomycin in compoundfree medium for various times. MALT1mut/mut patient and unaffected donor CD4+ T cells (1 × 106 cells) are pretreated with 2 μM MLT-748 for 24 h, compound is washed out over 2 h, and cells are then stimulated with PMA/ionomycin for various times up to 1 h.

Chemical Information & Solubility

Molecular Weight 492.32 Formula

C19H19Cl2N9O3
CAS No. 1832578-30-9 SDF --
Smiles CC(C(C1=C(C=NC2=CC(=NN21)Cl)NC(=O)NC3=CC(=C(N=C3)N4N=CC=N4)Cl)OC)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (199.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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