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关于此项目
经验公式(希尔记法):
C30H45N5O7S · xHCl
化学文摘社编号:
分子量:
619.77 (free base basis)
MDL number:
UNSPSC Code:
12352101
NACRES:
NA.22
Assay:
≥95%
Form:
powder or crystals
ligand
VH032
Quality Segment
assay
≥95%
form
powder or crystals
reaction suitability
reactivity: carboxyl reactive, reagent type: ligand-linker conjugate
functional group
amine
storage temp.
2-8°C
SMILES string
O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCOCCOCCN)=O)=O.Cl
InChI key
ZOYHUTRHKHRRPK-QVRKWNSCSA-N
Application
Protein degrader builiding block (S,R,S)-AHPC-PEG3-NH2 (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)
Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)
Other Notes
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation
Targeted Protein Degradation by Small Molecules
Impact of linker length on the activity of PROTACs
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation
Targeted Protein Degradation by Small Molecules
Impact of linker length on the activity of PROTACs
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
