2245237-53-8
Chemical Structure
VUBI1
Synonym(s): SOS1 activator 1
- CAS No.: 2245237-53-8
- Formula:C26H32ClFN6
- Molecular Weight:483.02
IUPAC Name: 6-chloro-1-(4-fluoro-3,5-dimethylbenzyl)-4-(4-methylpiperazin-1-yl)-2-(2,6-diazaspiro[3.3]heptan-2-yl)-1H-benzo[d]imidazole
InChIKey: JWZAQUXBYYOGFA-UHFFFAOYSA-N
SMILES: CN1CCN(C2=C3C(N(CC4=CC(C)=C(F)C(C)=C4)C(N5CC6(CNC6)C5)=N3)=CC(Cl)=C2)CC1
Biological Activity: 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].
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VUBI1 | 98.21% | 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. | ||||||||||||||||||||
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VUBI1 (Standard) | ≥98% | VUBI1 (Standard) is the analytical standard of VUBI1 (HY-111671). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [3]. Stickler S, et al. Targeting KRAS in pancreatic cancer. Oncol Res. 2024 Apr 23;32(5):799-805. [Content Brief]
- [4]. Hamilton G, et al. Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras. Curr Pharm Des. 2023;29(22):1741-1746. [Content Brief]
