Cas No.: | 1832578-30-9 |
Chemical Name: | MLT-748 |
Synonyms: | MLT-748;US9815842, Example 98;BDBM355974;1-(5-chloro-6-(2H- 1,2,3-triazol-2- yl)pyridin-3-yl)-3-(2- chloro-7-((1R,2R)- 1,2- dimethoxypropyl)py- razolo[1,5- a]pyrimidin-6-yl)urea;1-(5-chloro-6-(2H-1,2,3-triazol-2-yl)pyridin-3-yl)-3-(2-chloro-7-((1R,2R)-1,2-dimethoxypropyl)pyrazolo[1,5-a]pyrimidin-6-yl)urea;1-[2-Chloro-7-[(1R,2R)-1,2-dimethoxypropyl]pyrazolo[1,5-a]pyrimidin-6-yl]-3-[5-chloro-6-(triazol-2-y |
SMILES: | ClC1C=C2N=CC(=C([C@H]([C@@H](C)OC)OC)N2N=1)NC(NC1C=NC(=C(C=1)Cl)N1N=CC=N1)=O |
Formula: | C19H19Cl2N9O3 |
M.Wt: | 492.318660020828 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MLT-748 (MLT748) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 5 nM, does not show inhibitory activity against 22 other tested human proteases (IC50>100 uM); binds MALT1 in the allosteric Trp580 pocket, reversibly binds and stabilizes human mutant MALT1-W580S with Kd of 13 nM, with affinity similar to that of the wild type MALT1 (Kd=42 nM); stabilizes MALT1-W580S in MALT1mut/mut B cells with EC50 of 69 nM, blocks cleavage of MALT1 substrates in human lymphocytes, including HOIL1, RelB, CYLD, and BCL10 (BCL10 cleavage IC50=31 nM), rescues MALT1 function in patient MALT1mut/mut lymphocytes. |