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Thalidomide-O-amido-C4-NH2

Catalog No. T17818 CAS 1799711-24-2

Synonyms: E3 Ligase Ligand-Linker Conjugates 19, Cereblon Ligand-Linker Conjugates 6

Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6) is a synthesized ligand-linker conjugate that combines a Thalidomide-based cereblon ligand with a linker. It functions as an E3 ligase ligand-linker conjugate and finds applications in the synthesis of PROTACs[1].

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Thalidomide-O-amido-C4-NH2 Chemical Structure

Thalidomide-O-amido-C4-NH2, CAS 1799711-24-2

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Description

In vitro

Thalidomide-O-amido-C4-NH2, also known as Compound 41, serves as an amine intermediate in the synthesis of heterobifunctional PROTAC BET degraders. These degraders target the bromodomain and extra-terminal (BET) family of proteins—BRD2, BRD3, BRD4, and BRDT—which are crucial in gene transcription regulation and are attractive therapeutic targets for cancer and other diseases. Utilizing the proteolysis targeting chimera (PROTAC) approach, these small molecules induce the degradation of BET proteins. Specifically, Thalidomide-O-amido-C4-NH2 functions as a degron-linker (Compound DL6-TL), a structure that covalently links a degron to a targeting ligand. The degron binds to an E3 ubiquitin ligase (e.g., cereblon), facilitating the targeted degradation of the protein(s) bound by the targeting ligand.

Synonyms	E3 Ligase Ligand-Linker Conjugates 19, Cereblon Ligand-Linker Conjugates 6
Molecular Weight	402.4
Formula	C19H22N4O6
CAS No.	1799711-24-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins withPicomolar Cellular Potencies and Capable of Achieving Tumor Regression.J Med Chem. 2018 Jan 25;61(2):462-481. 2. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.

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Keywords

Thalidomide-O-amido-C4-NH2 1799711-24-2 Others E3 Ligase Ligand-Linker Conjugates 19 Thalidomide O amido C4 NH2 Cereblon Ligand-Linker Conjugates 6 Thalidomide-O-amido-C-4-NH2 ThalidomideOamidoC4NH2 inhibitor inhibit

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