MLT-748 |CAS:1832578-30-9 Probechem Biochemicals

Chemical Structure : MLT-748

CAS No.: 1832578-30-9

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MLT-748 (MLT748;MLT 748)

货号: 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).

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5 mg	￥2780	In stock
10 mg	￥4580	In stock
25 mg	￥7580	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	492.321
分子式	C19H19Cl2N9O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

1. Quancard J, et al. Nat Chem Biol. 2019 Jan 28. doi: 10.1038/s41589-018-0222-1.

MLT-748 (MLT748;MLT 748)

生物&药学活性

物理化学性质&存储条件

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MLT-748 (MLT748;MLT 748)

生物&药学活性

物理化学性质&存储条件

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