Category: Cancer

Balixafortide is a Selective and Well-Tolerated Peptidic CXCR4 Antagonist

Despite the introduction of new targeted therapies and cytotoxic agents, chemotherapy-pretreated metastatic breast cancer (MBC) remains an essentially incurable disease with only moderate median overall survival (OS). over 20 human tumor types overexpress C-X-C chemokine receptor type 4 (CXCR4). CXCR4 levels correlate with aggressive metastatic phenotypes and negative prognosis...

CID-1067700 is a Ras GTPases pan-Inhibitor with High Efficacy Towards Rab7

Alteration of small GTPase functions is a hallmark of genetic and sporadic human diseases, making GTPase family members attractive though understudied targets. Specifically, the Ras superfamily of GTPases includes Arf, Rho, Ras and Rab GTPase subfamilies. Besides, they regulate a broad range of cellular processes ranging from membrane trafficking...

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...

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...

CNX-500 is a Covalent Btk Inhibitor (CC-292) Linked to Biotin Chemically

Bruton’s tyrosine kinase (Btk) is a kinase. B cells and myeloid cells expressed exclusively. It plays a vital role in B cells. Btk plays an essential role in the B cell receptor (BCR) signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn...

BAY-474, a SGC Epigenetic Probe, is a Tyrosine-Protein Kinase c-Met Inhibitor

Potent, selective and broadly characterized small molecule modulators of protein function (chemical probes) are powerful research reagents. Genetic approaches are used to suppress the expression of the respective gene/protein. However, these methods have some deficiencies in drug discovery. They commonly remove or suppress the entire protein and they are...