1950634-92-0

Usage

Uses

Used in Pharmaceutical Industry:
dBET6 is used as a therapeutic agent for the treatment of various cancers. Its ability to selectively target and degrade BET proteins makes it a potential treatment option for patients with cancers driven by the dysregulation of these proteins. The use of dBET6 may help to inhibit tumor growth and progression, offering a new approach to cancer therapy.
Used in Cancer Research:
dBET6 is used as a research tool to study the role of BET proteins in cancer development and progression. By understanding the molecular mechanisms underlying the antitumor activity of dBET6, researchers can gain valuable insights into the pathogenesis of cancer and identify potential targets for the development of novel therapeutic strategies.
Used in Drug Development:
dBET6 serves as a lead compound in the development of new drugs targeting the BET protein family. Its potent and selective degradation of BET proteins can be leveraged to design and optimize new molecules with improved pharmacological properties, potentially leading to the discovery of more effective cancer treatments.

Upstream product

• 202592-23-2 (S)-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid 
• 1268524-70-4 (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate 
• 373-44-4 1,8-diaminooctan 
• 88829-82-7 tert-butyl N-(8-aminooctyl)carbamate 
• 852526-11-5 tert-butyl (8-(2-chloroacetamido)octyl)carbamate 
• 37418-88-5 3-hydroxyphthalic anhydride 
• 5054-59-1 4-Hydroxythalidomide 
• 1061605-21-7 2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}acetic acid 

Relevant academic research and scientific papers

HETEROBIFUNCTIONAL COMPOUNDS WITH IMPROVED SPECIFICITYFOR THE BROMODOMAIN OF BRD4

Disclosed are heterobifunctional compounds that effectuate selective degradation of a target protein, and which include a targeting ligand that binds a target protein and at least one other protein, a ligand that binds an E3 ubiquitin ligase or a component of E3 ubiquitin ligase, and a specificity modulating linker that links the first ligand and the second ligand. Pharmaceutical compositions containing the compounds, and methods of using and making the compounds are also disclosed.

REGULATING CHIMERIC ANTIGEN RECEPTORS

This invention is in the area of compositions and methods for regulating chimeric antigen receptor immune effector cell, for example T-cell (CAR-T), therapy to modulate associated adverse inflammatory responses, for example, cytokine release syndrome and tumor lysis syndrome, using targeted protein degradation.

TUNABLE ENDOGENOUS PROTEIN DEGRADATION WITH HETEROBIFUNCTIONAL COMPOUNDS

The present invention provides a means to modulate gene expression in vivo in a manner that avoids problems associated with CRISPR endogenous protein knock-out or knock-in strategies and strategies that provide for correction, or alteration, of single nucleotides. The invention includes inserting into the genome a nucleotide encoding a heterobifunctional compound targeting protein (dTAG) in-frame with the nucleotide sequence of a gene encoding an endogenously expressed protein of interest which, upon expression, produces an endogenous protein-dTAG hybrid protein. This allows for targeted protein degradation of the dTAG and the fused endogenous protein using a heterobifunctional compound.

METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to nucleic acids, polypeptides, cells, and methods for highly regulated, targeted degradation of proteins through the use of the bifunctional compounds.

METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.