MS-553

MS-553 is an orally administered, highly selective, non-covalent small molecule inhibitor of the beta isoform of protein kinase C (PKCβ). It is being developed primarily for the treatment of hematologic malignancies, especially chronic lymphocytic leukemia (CLL) and various B-cell lymphomas. The drug acts by inhibiting PKCβ activity, a key component in B cell receptor (BCR) signaling pathways that are critical for survival and proliferation of malignant B cells. Preclinical studies have shown that MS-553 reduces phosphorylation of PKCβ and its downstream targets such as GSK3β, ERK, IκBα, β-Catenin, Cyclin D2, and cMyc. This leads to decreased cell viability in CLL cells—including those with resistance mutations to Bruton’s tyrosine kinase inhibitors—and reduced production of pro-inflammatory cytokines like CCL3 and CCL4. Clinical trials are ongoing or planned for relapsed/refractory CLL/SLL and multiple subtypes of non-Hodgkin's lymphoma[1][2][3][4][5][6][7][8].

Other names

PKC-beta inhibitor MS-553