JH-X-119-01

JH-X-119-01 is a covalent inhibitor of IL-1 receptor-associated kinase 1 (IRAK1, IC50 = 9 nM). It is selective for IRAK1 over IRAK4 (IC50 = >10,000 nM). JH-X-119-01 is cytotoxic against a panel of mutant MyD88-expressing Waldenstrom's macroglobulinemia (WM), ABC subtype diffuse large B cell lymphoma (DLBCL), and lymphoma cells (EC50s = 0.59-9. µM). It has a synergistic cytotoxic effect in MyD88-mutant-expressing BCWM. WM and TMD8 ABC DLBCL cells when used in combination with ibrutinib (Cay-16274). JH-X-119-01 (5 and 10 mg/kg) also reduces lung injury and increases survival in a mouse model of LPS-induced sepsis.. Solulibility: DMSO: Sparingly soluble: 1-10 mg/mL: PBS (pH 7.2): Insouble.