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Thalidomide-O-amido-C4-NH2 hydrochloride

Catalog No. T18815 CAS 2245697-86-1

Thalidomide-O-amido-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that combines the cereblon ligand derived from Thalidomide with a linker. It is commonly employed in the synthesis of PROTACs[1].

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Thalidomide-O-amido-C4-NH2 hydrochloride Chemical Structure

Thalidomide-O-amido-C4-NH2 hydrochloride, CAS 2245697-86-1

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Description

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	438.86
Formula	C19H23ClN4O6
CAS No.	2245697-86-1

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 hydrochloride 2245697-86-1 Others Thalidomide-O-amido-C4-NH2 Hydrochloride ThalidomideOamidoC4NH2 hydrochloride Thalidomide-O-amido-C-4-NH2 hydrochloride Thalidomide O amido C4 NH2 hydrochloride inhibitor inhibit

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