929352
(S,R,S)-AHPC-di-trimethylamide-dioxodisulfide-carbonate ester
别名:
S-(1-(((((3R,5S)-1-((S)-2-((tert-butoxycarbonyl)amino)-3,3-dimethylbutanoyl)-5-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-3-yl)oxy)carbonyl)oxy)-2-methylpropan-2-yl) methanesulfonothioate
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关于此项目
ligand
VH032
Quality Segment
assay
≥95%
form
powder
functional group
disulfide
storage temp.
2-8°C
SMILES string
CC(C)(C)OC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)OC(OCC(C)(C)SS(C)(=O)=O)=O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O
InChI
1S/C33H48N4O9S3/c1-20-25(47-19-35-20)22-13-11-21(12-14-22)16-34-27(38)24-15-23(45-30(41)44-18-33(8,9)48-49(10,42)43)17-37(24)28(39)26(31(2,3)4)36-29(40)46-32(5,6)7/h11-14,19,23-24,26H,15-18H2,1-10H3,(H,34,38)(H,36,40)/t23-,24+,26-/m1/s1
InChI key
AZAVKYSXGOPVNY-RMTZWNOUSA-N
Application
Protein degrader building block (S,R,S)-AHPC-di-trimethylamide-dioxodisulfide-carbonate ester enables the synthesis of molecules for degradation of proteins and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a pendant disulfide, linked via a carbonate group. The pendant disulfide allows for targeted degradation of antibodies. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Other Notes
Targeted Protein Degradation by Small Molecules
Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
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
存储类别
11 - Combustible Solids
wgk
WGK 3