E3 Ligand-Linker Conjugate 3(E3 Ligase Ligand-Linker Conjugates 19)

Cas No.:	1799711-24-2
Chemical Name:	N-(4-Aminobutyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide
Synonyms:	E3 Ligase Ligand-Linker Conjugates 19;E3 Ligand-Linker Conjugate 3;Cereblon Ligand-Linker Conjugates 6;Thalidomide-O-amido-C4-NH2;Acetamide, N-(4-aminobutyl)-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-;N-(4-aminobutyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide
SMILES:	C(NCCCCN)(=O)COC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O
Formula:	C19H22N4O6
M.Wt:	402.401184558868
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.

Description:	E3 Ligand-Linker Conjugate 3(E3 Ligase Ligand-Linker Conjugates 19) is a degron-linker. The PROTAC linker is bound lo at least one targeting ligand.
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:	[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. 2017 Mar 24. [2]. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.