Name | E3 Ligase Ligand-Linker Conjugates 19 |
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Description | E3 Ligase Ligand-Linker Conjugates 19 is a degron-linker. The PROTAC linker is bound lo at least one targeting ligand. |
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Related Catalog | |
In Vitro | E3 Ligase Ligand-Linker Conjugates 19 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]. E3 Ligase Ligand-Linker Conjugates 19 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 |
Molecular Formula | C19H22N4O6 |
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Molecular Weight | 402.4 |
Hazard Codes | Xi |
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