2245237-53-8
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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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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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Antihistamine-1 (Standard) | ≥98% | Antihistamine-1 (Standard) is the analytical standard of Antihistamine-1 (HY-100238). This product is intended for research and analytical applications. Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively. | ||||||||||||||||||||
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(4S)-PROTAC SOS1 degrader-1 | (4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers. | |||||||||||||||||||||
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TRPC6-IN-2 | The compound inhibits TRPC proteins, and more specifically inhibits the TRPC6 protein. | |||||||||||||||||||||
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PROTAC SOS1 degrader-1 | PROTAC SOS1 degrader-1 is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers. | |||||||||||||||||||||
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TRPV4 antagonist 4 | TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury. | |||||||||||||||||||||
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VUBI1 analogue-1 | 98.94% | VUBI1 analogue-1 is a structural analog of VUBI1 (HY-111671), and also a key synthetic intermediate for the synthesis of SOS1 activators. VUBI1 analogue-1 can be used to synthesize (4S)-PROTAC SOS1 degrader-1 (HY-144657) for cancer-related research. | ||||||||||||||||||||
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iPAF1C | 99.91% | iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4+T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders). | ||||||||||||||||||||
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SOS1 activator 2 | SOS1 activator 2 (Compound 65) is a benzimidazole derivative and a SOS1 activator. SOS1 activator 2 has a high binding affinity for SOS1 with a Kd of 9 nM. SOS1 activator 2 can regulate the Ras-ERK signaling pathway, which can be used in the study of cancer. | |||||||||||||||||||||
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Mizolastine dihydrochloride | Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial. | |||||||||||||||||||||
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Mizolastine (Standard) | ≥98% | Mizolastine (Standard) is the analytical standard of Mizolastine. This product is intended for research and analytical applications. Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial. | ||||||||||||||||||||
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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]
