Stemcell, 100-1656, SB590885

Inhibit ERK phosphorylation and cell proliferation in cancer cells with SB590885, a potent inhibitor of B-Raf kinase (BRAF; Kd = 300 pM). BRAF is a key component in the extracellular signal-regulated kinase (ERK); a group of mitogen-activated protein kinase (MAPK) pathways (Takle et al. Bioorg Med Chem Lett, 2006), and mutations in the BRAF regulatory domain have been shown to increase kinase activity and maintain tumorigenicity of melanoma and other cancers. SB590885 influences this process by competitively binding the ATP-binding domain of BRAF, which selectively inhibits BRAF kinase activity (King et al. Cancer Res, 2006; Roskoski. Biochem Biophys Res Commun, 2010).

SB590885 has been used for:

CANCER RESEARCH

· Disrupt endolysosomal pathways, resulting in accumulation of acidic vacuole-like vesicles and sensitizing human melanoma cell lines to endoplasmic reticulum stress (Palušová et al. Cancers, 2020).

· Inhibit ERK phosphorylation, cell proliferation, and anchorage-independent growth of human melanoma cell lines and reduce tumor growth in a mouse xenograft model (King et al. Cancer Res, 2006).

DISEASE MODELING

· Induce hypertrophy in rat cardiomyocytes and promote cardiac hypertrophy in vivo in a mouse model (Clerk et al. Biochem J, 2022).