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Chemical Structure : MLT-748
CAS No.: 1832578-30-9
Catalog No.: PC-36042Not For Human Use, Lab Use Only.
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $278 | In stock | |
| 10 mg | $458 | In stock | |
| 25 mg | $758 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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).
MLT-748 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).
MLT-748 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).
MLT-748 rescues MALT1 function in patient MALT1mut/mut lymphocytes.
| M.Wt | 492.321 | |
| Formula | C19H19Cl2N9O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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 |
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1. Quancard J, et al. Nat Chem Biol. 2019 Jan 28. doi: 10.1038/s41589-018-0222-1.
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