hras 1

Hras-1Y i-motif Probe-1 is a probe of the hras-1Y i-motif which selectively and directly interacts with it.

AMG410是一种非共价、双态GDP（OFF）和GTP（ON）结合的泛KRAS抑制剂，Kd (GDP) = 1 nM，Kd (GTP) = 22 nM，从而能够和循环无关地阻断KRAS。AMG410对KRAS的选择性超过HRAS和NRAS2的100倍，与KRAS G12C抑制剂结合在相同的变烯袋上，并且在KRAS G12D，G12V, G12C，G13D和其他突变体中具有高效力，IC 50 = 1-4 nM，能够在KRAS突变的结肠直肠、胰腺和肺模型中使肿瘤消退并且降低磷酸化的ERK水平。

RAS inhibitor Abd-7 is a powerful compound (Kd=51 nM) that binds to RAS and inhibits the protein-protein interaction (PPI) between RAS and its effectors. By interacting with RAS within cells, RAS inhibitor Abd-7 hinders RAS-effector interactions and suppresses endogenous RAS-dependent signaling. Additionally, RAS inhibitor Abd-7 disrupts the PPI of different mutant KRAS proteins with PI3K, CRAF, RALGDS, as well as NRAS Q61H and HRAS G12V[1].