VUBI1

VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer[1][2][3][4].

Product Specifications

CAS Number

[2245237-53-8]

Product Name Alternative

SOS1 activator 1

UNSPSC

12352005

Target

Ligands for Target Protein for PROTAC; PERK; Ras; SOS1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein; MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sos1-activator-1.html

Concentration

10mM

Purity

98.01

Solubility

DMSO : 10 mg/mL (ultrasonic)

Smiles

CN1CCN(C2=C3C(N(CC4=CC(C)=C(F)C(C)=C4)C(N5CC6(CNC6)C5)=N3)=CC(Cl)=C2)CC1

Molecular Formula

C26H32ClFN6

Molecular Weight

483.02

References & Citations

[1]Timothy R Hodges, et al. Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J Med Chem. 2018 Oct 11;61 (19) :8875-8894.|[2]Zhou C, et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022 Mar 10;65 (5) :3923-3942.|[3]Stickler S, et al. Targeting KRAS in pancreatic cancer. Oncol Res. 2024 Apr 23;32 (5) :799-805.|[4]Hamilton G, et al. Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras. Curr Pharm Des. 2023;29 (22) :1741-1746.