ML141 is a Selective, Reversible and Non-competitive Cdc42 GTPase Inhibitor

Cdc42 protein is an essential GTPase that belongs to the Rho/Rac subfamily of Ras-like GTPases. These proteins act as molecular switches to activate downstream components of a biological pathway. CDC42 plays an important role in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Particularly, Overactive Cdc42 implicates...

ZCL278 is a Selective Cdc42 Inhibitor, with Antiviral Activity

Cdc42 is a member of the Rho GTPase family of low molecular weight G proteins. It is an important regulator of many biological processes. Besides, Cdc42 plays key roles in cytoskeletal organization, vesicular trafficking, cell cycle control, and transcription. As with most GTPases, transduction of signals occurs through the...

ZLDI-8, an ADAM-17 and Notch Inhibitor, Enhances Chemotherapeutic Effects

ADAM metallopeptidase domain 17 (ADAM17) is an enzyme that belongs to the ADAM protein family of metalloproteases. ADAM17 plays a prominent role in the Notch signaling pathway. In this study, researchers demonstrated the discovery of ZLDI-8. ZLDI-8 is a novel inhibitor for Notch activating/cleaving enzyme ADAM-17. In particular, ZLDI-8...

BTSA1 is a High Affinity and Orally Active BAX Activator

The BCL-2 family protein BAX is a central mediator of apoptosis. Besides, overexpression of anti-apoptotic BCL-2 proteins contributes to tumor development and resistance to therapy by suppressing BAX and its activators. Cancer cells depend on their ability to enforce cell survival pathways and block cell death mechanisms. Moreover, pro-apoptotic...

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...