sevenless

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

SOS2 ligand 1 (compound 2) is a selective ligand for son of sevenless 2 (SOS2), exhibiting a KD value of 4.6 µM.

SOS1-IN-18 (Compound 8) is an inhibitor of the Son of Sevenless 1 protein (SOS1) with a dissociation constant (KD) of 2.6 nM. It disrupts the SOS1-KRAS G12C interaction with an IC50 of 3.4 nM, inhibits ERK phosphorylation in H358 cells with an IC50 of 31 nM, and curtails the proliferation of H358 cells with an IC50 of 5 nM.

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.

ASP2453 is a potent, selective, and covalent inhibitor of KRAS G12C that inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.

SOS1-IN-3 is an effective inhibitor of SOS1 (son of sevenless homolog 1) (IC50=5 nM). SOS1-IN-3 shows antitumor activity.

SOS1-IN-13 is a potent inhibitor of son of sevenless homolog 1 (SOS1), displaying IC50 values of 6.5 nM for SOS1 and 327 nM for pERK. SOS1-IN-13 holds significant research value in anticancer studies.

SOS1 agonist-1 (compound 79) serves as an agonist for the Son of sevenless homologue 1 (SOS1), a crucial guanine nucleotide exchange factor involved in catalyzing the GDP to GTP exchange on RAS proteins, thus regulating RAS activation. By increasing nucleotide exchange on RAS, SOS1 agonists enhance cellular RAS-GTP levels and induce biphasic signaling alterations in ERK1/2 phosphorylation, playing a pivotal role in anti-cancer activity [1].

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. Display