SOS1

SOS1 inhibitors block the interaction through which son of sevenless 1 (SOS1) activates Ras proteins. SOS1 is a guanine nucleotide exchange factor that swaps guanosine diphosphate (GDP) for guanosine triphosphate (GTP) on Ras. BAY 293 was described in 2019 as blocking Ras activation by disrupting the interface between SOS1 and Kirsten rat sarcoma viral oncogene homolog (KRAS). BI-3406 followed as a selective SOS1-KRAS interaction inhibitor studied in KRAS-driven cell models together with inhibition of mitogen-activated protein kinase kinase (MEK). MRTX0902 extends the same series, while PROTAC SOS1 degrader-1 TFA removes the protein instead of blocking the interface. VUBI1 acts in the opposite direction as a reported SOS1 activator.

2 Items

  • VUBI1
    Cat. No.
    A24569

    VUBI1 (SOS1 activator 1)

    Synonyms: SOS1 activator 1

    VUBI1 (SOS1 Activator 1) is a benzimidazole-derived small molecule that acts as a potent activator of the guanine nucleotide exchange factor SOS1, with a dissociation constant (Kᴅ) of 44 nM. It promotes RAS activation by enhancing RAS-GTP formation and modulates downstream ERK phosphorylation, thereby influencing RAS–MAPK signaling. In addition, VUBI1 serves as a functional ligand for the development of PROTAC-based degraders, such as PROTAC SOS1 Degrader-1, to induce targeted SOS1 degradation. VUBI1 is a valuable compound for studying RAS pathway regulation and its role in cancer biology.

    1 mg
    $315.00
    5 mg
    $945.00
    All 4 sizes
  • SOS1 activator 2
    Cat. No.
    A36714

    SOS1 activator 2

    SOS1 Activator 2 engages the SOS1 protein, functioning as a potent activator with a binding affinity characterized by a Kd of 9 nM. By modulating the Ras-ERK signaling pathway, SOS1 Activator 2 serves as a valuable tool in cancer research, facilitating investigations into signal transduction mechanisms and potential therapeutic strategies. Its specificity and efficacy make it an essential reagent for studies aimed at understanding the complexities of oncogenic signaling pathways.

    Out of stock

    All 3 sizes

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