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MLT-748 is a potent and selective allosteric inhibitor of MALT1 with an IC50 of 5 nM. By substituting Trp580, MLT-748 binds to the interface between the caspase and immunoglobulin (Ig3) domains and locks the catalytic site to an inactive state.
Brand: BCM
Target: MALT1
In Vitro: MLT-748 (2 μM, 24 hours) enhances the phosphorylation of p65 and IκBα in MALT1mut/mut patient immortalized B cells. MLT-748 (0-2 μM) stabilizes cellular MALT1-W580S (EC50: 69 nM). MLT-748 reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with an affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM).
pKa: 7.78±0.46(Predicted)
Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.
Isomeric SMILES: C[C@H]([C@@H](C1=C(C=NC2=CC(=NN21)Cl)NC(=O)NC3=CC(=C(N=C3)N4N=CC=N4)Cl)OC)OC
InChIKey: XKQLNDPUQSZBJW-QGHHPUGFSA-N
InChI: InChI=1S/C19H19Cl2N9O3/c1-10(32-2)17(33-3)16-13(9-22-15-7-14(21)28-29(15)16)27-19(31)26-11-6-12(20)18(23-8-11)30-24-4-5-25-30/h4-10,17H,1-3H3,(H2,26,27,31)/t10-,17+/m1/s1
Attribute [Chem Name] 1-[2-chloro-7-[(1R,2R)-1,2-dimethoxypropyl]pyrazolo[1,5-a]pyrimidin-6-yl]-3-[5-chloro-6-(triazol-2-yl)pyridin-3-yl]urea [Synonym] MLT-748 [CAS No.] 1832578-30-9 [MDL No.] MFCD31813802 [Formula] C19H19Cl2N9O3 [Molecular] 492.32 [Form] Solid Powder [Storage] Store at -20°C
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