2143475-98-1

Usage

Uses

Used in Pharmaceutical Industry:
N-(2-(9H-carbazol-1-yl)phenyl)acetamide is used as a potential pharmaceutical compound for its possible anti-cancer properties, given the known biological activities of acetamide derivatives and the anti-cancer studies on carbazole derivatives.
Used in Organic Synthesis:
In the field of organic synthesis, N-(2-(9H-carbazol-1-yl)phenyl)acetamide serves as a valuable intermediate or reactant due to its unique structure and reactivity.
Used in Dyes and Pigments Industry:
N-(2-(9H-carbazol-1-yl)phenyl)acetamide is used as a component in dyes and pigments, taking advantage of its tricyclic aromatic carbazole moiety to impart color and stability to these products.

Upstream product

• 380430-61-5 N-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetamide 
• 16807-11-7 1-bromo-9H-carbazole 
• 169760-16-1 2-acetamidophenylboronic acid 

Relevant academic research and scientific papers

Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14

Macrodomains are conserved protein interaction modules that can be found in all domains of life including in certain viruses. Macrodomains mediate recognition of sequence motifs harboring adenosine diphosphate ribose (ADPR) modifications, thereby regulating a variety of cellular processes. Due to their role in cancer or viral pathogenesis, macrodomains have emerged as potential therapeutic targets, but the unavailability of small molecule inhibitors has hampered target validation studies so far. Here, we describe an efficient screening strategy for identification of small molecule inhibitors that displace ADPR from macrodomains. We report the discovery and characterization of a macrodomain inhibitor, GeA-69, selectively targeting macrodomain 2 (MD2) of PARP14 with low micromolar affinity. Co-crystallization of a GeA-69 analogue with PARP14 MD2 revealed an allosteric binding mechanism explaining its selectivity over other human macrodomains. We show that GeA-69 engages PARP14 MD2 in intact cells and prevents its localization to sites of DNA damage.

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2

The polyadenosine-diphosphate-ribose polymerase 14 (PARP14) has been implicated in DNA damage response pathways for homologous recombination. PARP14 contains three (ADP ribose binding) macrodomains (MD) whose exact contribution to overall PARP14 function in pathology remains unclear. A medium throughput screen led to the identification of N-(2(-9H-carbazol-1-yl)phenyl)acetamide (GeA-69, 1) as a novel allosteric PARP14 MD2 (second MD of PARP14) inhibitor. We herein report medicinal chemistry around this novel chemotype to afford a sub-micromolar PARP14 MD2 inhibitor. This chemical series provides a novel starting point for further development of PARP14 chemical probes.