E3 Ligase Ligand-Linker Conjugates 19
Names
[ CAS No. ]:
1799711-24-2
[ Name ]:
E3 Ligase Ligand-Linker Conjugates 19
Biological Activity
[Description]:
E3 Ligase Ligand-Linker Conjugates 19 is a degron-linker. The PROTAC linker is bound lo at least one targeting ligand.
[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]
[Related Small Molecules]
(+)-JQ1
|
GSK126
|
Tazemetostat (EPZ-6438)
|
Birabresib (OTX015)
|
A 485
|
Curcumin
|
ARV-771
|
ARV-825
|
I-BET762
|
BI 2536
|
GSK343
|
C646
|
3-Deazaneplanocin A (hydrochloride)
|
I-BET151
|
666-15
Chemical & Physical Properties
[ Molecular Formula ]:
C19H22N4O6
[ Molecular Weight ]:
402.4
Safety Information
[ Hazard Codes ]:
Xi