ras/erk activation

XRP44X (XRP 44X) 是Ras 诱导的转录激活的抑制剂，IC50为 10 nM，通过 FGF-2 抑制 Ras-Erk-1 2 通路激活。它抑制Elk3。它还对微管有影响。

UC-857993 是一种选择性SOS1-Ras 抑制剂 (Kd=14.7 μM, His6-SOS1cat)，抑制其催化活性。UC-857993 还能抑制ERK 和Ras 激活，抑制小鼠胚胎成纤维细胞 (MEF) 的生长。

Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras Raf ERK p53 pathway. (20Z) -Pseudoginsenoside Rh2 and (20E)-Pseudoginsenoside Rh2 have antioxidative activity.

POP-3MB (compound 1b) 是一种ICMT抑制剂 (IC50: 2.5 μM)，能够改变K-Ras的亚细胞定位，并抑制Ras的活化。此外，POP-3MB 还能抑制Erk的磷酸化。

Son of sevenless homolog 1 (Sos1) is a guanine nucleotide exchange factor (GEF) that directs the exchange of Ras-GDP to Ras-GTP by binding to SH3 domains of the growth factor receptor-bound protein 2 (Grb2), leading to the activation of ERK. Ras inhibitory peptide is a synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2. It specifically blocks the interaction of the GEF with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases, including epidermal growth factor receptor.

Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.