Werner syndrome helicase (WRN) is a key drug target for cancers with microsatellite instability.  To support the discovery of potent and selective WRN inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to support hit finding and lead optimization efforts targeting WRN.  Our panel of services also include high-quality WRN protein production …Read More >

As reported in Business Wire: DNA-Encoded Libraries (DELs) and NanoBRET Target Engagement Assays Accelerate Drug Discovery: “The authors demonstrate that DELs can benefit chemical biologists who require verification of live cell target engagement for their protein of interest. This is particularly beneficial for understudied protein classes that may not have existing chemical probes. Additionally, they …Read More >

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays. With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition …Read More >

WuXi AppTec scientists recently contributed to a research article in Cell Chemical Biology demonstrating the successful conversion of ligands identified from DNA-encoded library (DEL) screening into highly functional, cell-active, bioluminescence resonance energy transfer (BRET) probes. The authors show that analyzing preliminary DEL hits based on target occupancy data generated in live, intact cells is an …Read More >

To accelerate screening and lead optimization efforts involving immune cell differentiation, WuXi AppTec offers a comprehensive CD34+ hematopoietic stem cell differentiation platform.  Our panel includes neutrophil, eosinophil, erythroid, and mast cell differentiation, as well as monocyte/macrophage differentiation and polarization, and megakaryocyte/platelet differentiation. Check out our comprehensive platform of immune profiling and biomarker services

WuXi AppTec scientists collaborated on a study to characterize a series of pyrroloquinoline derivatives that were designed and synthesized to understand the effect of various substitutions on human cytomegalovirus (HCMV) polymerase activity, antiviral activity, and hERG inhibition.  Results suggest that substitutions can be fine-tuned to reduce hERG inhibition while maintaining HCMV antiviral potency. The abstract …Read More >

Learn how parallel medicinal chemistry (PMC) and high throughput experimentation (HTE) combined with machine learning can provide a more focused approach to target molecules, resulting in a more concentrated set of compounds to make the process of lead selection easier. Our experts show how PMC can shorten the turnaround time of the design-synthesis-test cycle, providing …Read More >

We offer an extensive panel of inflammatory bowel disease models in mice and rats, including genetically modified, chemically induced, and adoptive transfer-related IBD models. Let our experts help you choose the best IBD animal models to advance your research programs. Learn more about our platform of inflammation models  

Macrocyclic peptides are an emerging molecular class for targeting intracellular protein–protein interactions (PPIs) and for providing an oral modality for drug targets. Herein, we use DNA-encoded cyclic peptide libraries to discover a neutral nonapeptide, UNP-6457, that inhibits MDM2–p53 interaction with an IC50 of 8.9 nM. These studies showcase how tailored DEL libraries can directly yield …Read More >