MLT-748

Protein target name:

MALT1

Mechanism of action:

Allosteric inhibitor

Recommended Concentration for use in cells:

up to 2 uM

Probe Availability

MedChemExpress

Probe Information

Target and Probe Information

Target Details

Target class:

Other

Define other target class:

Paracaspase

Subclass:

Peptidase C14B

HUGO ID:

HGNC:6819

Entrez gene ID:

10892

UNIPROT ID:

Q9UDY8

Target alias:

MLT; MLT1; IMD12; PCASP1

Probe Details

Chemical Probes Portal ID:

CPP1867

PubChem CID:

129072285

SMILES string:

O=C(NC1=CC(Cl)=C(N2N=CC=N2)N=C1)NC3=C([C@@H](OC)[C@H](OC)C)N4C(N=C3)=CC(Cl)=N

InChi Key:

XKQLNDPUQSZBJW-QGHHPUGFSA-N

Physico-chemical properties

NMR:

1 H NMR (600 MHz, DMSO-d6) δ ppm: 10.54 (s, 1H), 8.92 (s, 1H), 8.56 (d, J = 2.3 Hz, 1H), 8.50 (d, J = 2.3 Hz, 1H), 8.39 (s, 1H), 8.16 (s, 2H), 6.96 (s, 1H), 5.28 (s, 1H), 3.87 (m, 1H), 3.32 (s, 3H), 3.21 (s, 3H), 1.24 (d, J = 5.8 Hz, 3H).

13C NMR (151 MHz, DMSO-d6) δ 153.34, 150.32, 146.34, 144.30, 141.53, 139.01, 136.81, 136.18, 127.33, 126.24, 121.89, 95.71, 80.47, 76.58, 58.05, 56.95, 14.97.

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50, KD

5 nM (IC50), 13 nM W580S, 42 nM WT

Potency assay:

MALT1 peptide cleavage inhibition, SPR

PDB ID for probe-target interaction (3D structure):

6H4A

Structure-activity relationship:

yes

Off target activity

Probe Selectivity in Vitro:

MLT-748 does not show inhibitory activity on any of 22 other tested human proteases with IC50 values >100 μM

In cell validation

On target activity in cells

Potency in cells:

EC50

69 nM

Potency assay (cells):

MALT1 Cleavage inhibition of BCL10, Immunoblotting densitometry

Target engagement assay (cells):

MLT-748 blocks cleavage of MALT1 substrates in human lymphocytes.

Primary Reference

Reference (doi):

10.1038/s41589-018-0222-1

Reference (PMID):

30692685

MLT-748

Probe Availability

Probe Information

Target Details

MLT; MLT1; IMD12; PCASP1

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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MLT-748

Probe Availability

Probe Information

Target Details

MLT; MLT1; IMD12; PCASP1

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?