SAH-SOS1A 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。 SAH-SOS1A 以纳摩尔级亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS（G12D、G12V、G12C、G12S 和 Q61H）结合，直接且独立地阻断核苷酸结合，削弱 KRAS 驱动的癌细胞活力，并通过机制阻断 KRAS 下游的 ERK-MAPK 磷酸信号级联发挥其作用。
货号:ajcx27892
CAS:1652561-87-9
分子式:C100H159N27O28
分子量：2187.53
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Displays cytotoxicity in KRas-driven cancer cell lines and inhibits downstream ERK-MAPK signaling. Cell permeable.

Leshchiner et al (2015) Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc.Natl.Acad.Sci.USA. 112 1761 PMID:25624485