SGR-1505 (SGR1505) is a highly potent, allosteric MALT1 (paracaspase 1, PCASP1) inhibitor with biochemical IC50 of 1.3 nM.
SGR-1505 shows excellent selectivity against a panel of 17 human proteases (all IC50 values >10 μM).
SGR-1505 also demonstrats high selectivity against a kinase profiling panel of 468 human kinases and disease-relevant mutant variants.
SGR-1505 shows high cellular potency in BCL10 cleavage, IL-10 secretion, and cell viability assays using ABC-DLBCL cell lines OCI-LY3 and OCI-LY10 (IC50=10-120 nM).
SGR-1505 inhibits luciferase activity of the NF-κB reporter in Jurkat cells with IC5 of 36 nM.
SGR-1505 displays potent IL-2 inhibition with an IC50 of 18 nM in activated T-cell cytokine secretion assays in human peripheral blood mononuclear cells (PBMCs).
SGR-1505 at 75 mg/kg (three times daily, TID) suppressed tumor growth in a dose-dependent manner in OCI-LY3 xenograft model.