Biological Activity
SAH-SOS1A is a 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.Technical Data
(Modifications: Arg-1 = N-terminal Ac, X = (S)-2-(4-pentenyl)alanine, X-7 and X-11 stapled together with a double bond)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Additional Information
Background References
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Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices.
Leshchiner et al.
Proc.Natl.Acad.Sci.USA., 2015;112:1761
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