SB-590885

SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer^[1][2][3]. IC50 & Target:IC50: 0.16 nM (B-Raf) In Vitro:SB-590885(1 μM; 12 d) increases the cell number by more than 10-fold compared with the control group in erythroid differentiation culture of UCB-CD34⁺ hematopoietic stem/progenitor cells, while transiently delaying the erythroid differentiation process^[1].
SB-590885(1 μM; 14 d) significantly increases the area of BFU-E erythroid colonies and the total number of erythroid cells, without affecting the proportion of colonies of other lineages. It also alleviates ineffective erythropoiesis caused by cytokine deprivation, reduces apoptosis, and promotes cell proliferation^[1].