MLT-748

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MLT-748 (MLT748) 是一种有效的、选择性的、MALT1 paracaspase 变构抑制剂，IC50 为 5 nM。

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.

Western Blot Analysis Cell Line:MALT1mut/mut patient immortalized B cells Concentration:2 μM Incubation Time:24 hours Result:Increased NF-κB signaling phosphorylation of both p65 and IκBα as early as 5 min after stimulation with PMA and ionomycin.

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MLT748 | MLT 748

Apoptosis

Caspase

Caspase

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1832578-30-9

492.321

C19H19Cl2N9O3

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (406.24 mM)

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)=N4

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

(-20℃)

With Ice Pack

≥ 2 years