MLT-748

For research use only.

Catalog No.S8898

MLT-748 Chemical Structure

CAS No. 1832578-30-9

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.

Purity & Quality Control

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

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 98 mg/mL (199.05 mM)
Ethanol 10 mg/mL (20.31 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 492.32
Formula

C19H19Cl2N9O3

CAS No. 1832578-30-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C(C1=C(C=NC2=CC(=NN21)Cl)NC(=O)NC3=CC(=C(N=C3)N4N=CC=N4)Cl)OC)OC

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID