Thalidomide-O-amido-C4-NH2 hydrochloride

Modify Date: 2024-01-10 12:30:10

Thalidomide-O-amido-C4-NH2 hydrochloride structure	Common Name	Thalidomide-O-amido-C4-NH2 hydrochloride
	CAS Number	2245697-86-1	Molecular Weight	438.86
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₉H₂₃ClN₄O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Thalidomide-O-amido-C4-NH2 hydrochloride

Thalidomide-O-amido-C4-NH2 hydrochloride, 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].

Name	Thalidomide-O-amido-C4-NH2 hydrochloride

Description	Thalidomide-O-amido-C4-NH2 hydrochloride, 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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PROTAC >> E3 Ligase Ligand-Linker Conjugate
Target	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].
References	[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.

Molecular Formula	C₁₉H₂₃ClN₄O₆
Molecular Weight	438.86

Hazard Codes	Xi