F1324 is a High Affinity BCL6 Peptidic Inhibitor

B cell lymphoma 6 (BCL6) is a transcriptional repressor that interacts with its corepressors BcoR and SMRT. Since this protein-protein interaction (PPI) induces activation and differentiation of B lymphocytes, BCL6 is an attractive drug target for potential autoimmune disease treatments. In addition, BCL6 acts as a master regulator of...

MSN-125 is a Potent Bax and Bak Oligomerization Inhibitor

Aberrant apoptosis can lead to acute or chronic degenerative diseases. Apoptosis largely divides into two pathways ultimately leading to caspase activation and subsequent cellular disintegration. Extracellular signals activating death receptors triggers the extrinsic pathway, and intracellular stress activates the intrinsic pathway. It largely regulated at the mitochondrial outer membrane...

BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor

c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...

BI-9321, a First-in-Class Chemical Probe, is a NSD3-PWWP1 Inhibitor

Post-translational modification of histones by histone-modifying enzymes represents a key element of epigenetic regulation. Epigenetic reader domains are structurally diverse. They include bromodomains, PHD domains, methyl-lysine- and/or methyl-arginine-binding domains, frequently co-locating within the same proteins. By interfering with the function of specific domains, selective chemical probes represent powerful tools...

AGN194204 is an Orally Active and Selective RXR Agonist

Rexinoids are selective ligands for the retinoid X receptors (RXRα, RXRβ, and RXRγ). Specifically, rexinoids are multifunctional drugs that are useful for both the prevention and treatment of lung and breast cancer in preclinical animal models. Besides, retinoid X receptors heterodimerize with other receptors in the nuclear receptor superfamily. They modulate the activities of numerous steroid-like...

6RK73 is a Covalent Irreversible and Specific UCHL1 Inhibitor

Approximately 90% of breast cancer-related deaths are due to metastasis. During the metastasis process, epithelial-mesenchymal transition (EMT) plays an important role. The secreted cytokine transforming growth factor-β (TGFβ) can induce it. Breast cancer has multiple subtypes with distinct metastatic potential based on genetic and clinical features. The most aggressive...

ADH-503 is an Orally Active and Allosteric CD11b Agonist

Integrin αMβ2 (CD11b/CD18) is a multifunctional integrin expressed on myeloid cells. In addition, CD11b/CD18 is an integrin molecule and plays an important role in their trafficking and cellular functions in inflamed tissues. Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal malignancy in which very limited responses to immunotherapy have been observed....