Name: SB747651A-PEG1-VH-032
Brand: BOC Sciences
Rating: 5 (1 reviews)

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IUPACName

(2S,4R)-1-((S)-2-(2-(2-(4-(((2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl)methyl)amino)piperidin-1-yl)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

InChI Key

JIBASKHLWXFKGZ-BZLMBYDGSA-N

InChI

InChI=1S/C42H56N12O6S/c1-6-53-35-28(19-44-21-31(35)48-39(53)34-38(43)51-60-50-34)20-45-29-11-13-52(14-12-29)15-16-59-23-33(56)49-37(42(3,4)5)41(58)54-22-30(55)17-32(54)40(57)46-18-26-7-9-27(10-8-26)36-25(2)47-24-61-36/h7-10,19,21,24,29-30,32,37,45,55H,6,11-18,20,22-23H2,1-5H3,(H2,43,51)(H,46,57)(H,49,56)/t30-,32+,37-/m1/s1

Mechanism

Target: SB747651A-PEG1-VH-032 is designed to target MSK1 kinase for VHL recruitment.

Binding site: Its SB747651A ligand binds the N-terminal ATP pocket of MSK1.

Mechanism of action: SB747651A-PEG1-VH-032 is a VHL-recruiting PROTAC scaffold built from the MSK1 inhibitor SB-747651A, a PEG1 linker, and the VHL ligand VH-032. Its design aims to test whether MSK1 engagement can be converted into VHL-dependent ubiquitination and proteasomal degradation. Compared with the pomalidomide analog, this construct enables evaluation of E3-ligase choice, linker geometry, and ternary-complex compatibility for MSK-family kinase degradation. It is suitable for structure-activity studies assessing target engagement, degradation selectivity, and VHL-mediated kinase turnover.

Applications

• PROTAC-Driven Protein Degradation: SB747651A-PEG1-VH-032 serves as a potent tool for the targeted degradation of specific proteins within cellular environments. It facilitates the recruitment of E3 ubiquitin ligases to proteins of interest, promoting their ubiquitination and subsequent proteasomal degradation, thus aiding in the study of protein function and regulation.

• Targeted Degradation in Signal Transduction: This PROTAC compound is instrumental in dissecting signaling pathways by selectively degrading signaling proteins. By enabling the controlled removal of target proteins, researchers can better understand the dynamics and interactions within complex signaling networks.

• Structural Biology via PROTACs: SB747651A-PEG1-VH-032 aids in elucidating protein structures by selectively degrading proteins that are challenging to study due to their transient nature or low abundance. This application enhances the ability to capture and analyze protein conformations and interactions.

• Functional Genomics with PROTACs: Utilizing SB747651A-PEG1-VH-032 in functional genomics studies allows for the precise manipulation of protein levels, thereby facilitating the identification of gene functions and interactions. This approach is invaluable for exploring the genetic basis of cellular processes and disease mechanisms.

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂