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Thalidomide-O-PEG2-carboxylic acid

目录号 数量 价格 提前通知时间
4192-25mg 25 mg $148 现货
4192-100mg 100 mg $480 现货
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Thalidomide-containing building block with PEG2-linker and carboxylic group for convenient PROTAC molecule assembly via conjugation with amino-functionalized linkers and target protein ligands. The carboxylic acid functional group should be activated with peptide coupling reagents like PyBOP or carbodiimides like EDC to form a stable amide linkage with amines. PEG2 is a hydrophilic linker providing a good separation between the parts of the PROTAC molecule.

Proteolysis targeting chimeras (PROTACs) are cell-permeable heterobifunctional molecules that can remove specific proteins from the cell. One end of such molecule contains a ligand to bind to the target, and the second end recruits the E3 ligase complex. Close proximity results in substrate polyubiquitination and subsequent protein degradation by cellular proteasome.

There are several types of E3 ligases that are practically suitable for such a purpose. Thalidomide is the ligand capable of recruiting Cereblon (CRBN) E3 ligase.

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Thalidomide-carboxylic acid

Thalidomide-containing building block with carboxylic acid functionality for convenient PROTAC molecule assembly by attachment amino-functionalized linkers and ligands to thalidomide via 4-O-position.
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Thalidomide-O-PEG2-azide

Thalidomide-containing building block with PEG2-linker and azide function group for conjugation with alkyne-functionalized linkers and target protein ligands through click chemistry reactions.
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General properties

Appearance: off-white solid
Molecular weight: 434.40
Molecular formula: C20H22N2O9
Solubility: in DMSO, DMF
Quality control: NMR 1H and HPLC-MS (95+%)
Storage conditions: 24 months after receival at -20°C in the dark. Transportation: at room temperature for up to 3 weeks. Desiccate.
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