MLT-748

Catalog No.S8898 Batch:S889801

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Technical Data

Formula

C19H19Cl2N9O3
Molecular Weight 492.32 CAS No. 1832578-30-9
Solubility (25°C)* In vitro DMSO 98 mg/mL (199.05 mM)
Ethanol 10 mg/mL (20.31 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.6mg/ml
5% DMSO 95% Corn oil
1.6mg/ml
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]
  • 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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.