1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugate
  3. Thalidomide-O-amido-C4-NH2

Thalidomide-O-amido-C4-NH2 (Synonyms: Cereblon Ligand-Linker Conjugates 6; E3 Ligase Ligand-Linker Conjugates 19)

Cat. No.: HY-107438
Handling Instructions

Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

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Thalidomide-O-amido-C4-NH2 Chemical Structure

Thalidomide-O-amido-C4-NH2 Chemical Structure

CAS No. : 1799711-24-2

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Description

Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].

IC50 & Target[1]

Cereblon

 

In Vitro

Thalidomide-O-amido-C4-NH2 is an amine intermediate (Compound 41), which can be used as is a heterobifunctional PROTAC BET degrader. The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-molecule BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation[1]. Thalidomide-O-amido-C4-NH2 is a degron-linker (refer to Compound DL6-TL). Degron-linker-targeting ligand, wherein the linker is covalently bound lo at least one degron and at least one targeting ligand, the degron is a compound capable of binding to an ubiquitin ligase such as an E3 ubiquitin ligase (e g, cereblon), and the targeting ligand is capable of binding to the targeted protein (s)[2].

Molecular Weight

402.40

Formula

C₁₉H₂₂N₄O₆

CAS No.

1799711-24-2

SMILES

NCCCCNC(COC1=C(C(N2C(CCC3=O)C(N3)=O)=O)C(C2=O)=CC=C1)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Thalidomide-O-amido-C4-NH2Cereblon Ligand-Linker Conjugates 6E3 Ligase Ligand-Linker Conjugates 19E3 Ligase Ligand-Linker ConjugateInhibitorinhibitorinhibit

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Thalidomide-O-amido-C4-NH2
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HY-107438
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