RA-9 is a Selective Proteasome-Associated DUBs Inhibitor

The ubiquitin-proteasome-system (UPS) is responsible for most of the intracellular protein degradation in eukaryotes. UPS consists of three components: the proteasomes, the ubiquitin conjugating system, and the deubiquitinating enzymes (DUBs). DUBs deconjugate ubiquitin from targeted proteins and this step is essential for protein degradation. The de-ubiquitination is required for...

MYLS22 is a Selective Optic Atrophy 1 (OPA1) Inhibitor

Optic neuropathy is damage to the optic nerve from any cause. Specifically, damage and death of these nerve cells, or neurons, leads to characteristic features of optic neuropathy. Angiogenesis requires an internal mitochondrial membrane mitochondrial fusion protein optic atrophy 1 (OPA1). Besides, mitochondrion fusion is controlled by mitochondrion fusion...

DI-82 is a Potent Deoxycytidine Kinase (dCK) Inhibitor with Anti-tumor Acitivity

Deoxycytidine kinase (dCK) is an enzyme that is encoded by the DCK gene in humans. Specifically, dCK mainly phosphorylates deoxycytidine (DC) and converts DC into deoxycytidine monophosphate. Mall molecule dCK inhibitor can combine pharmacological disturbance of the de novo dNTP biosynthesis pathway. Besides, it can eliminate the acute lymphoblastic...

JCN037 is a Non-Covalent and Brain-Penetrant EGFR Inhibitor

The epidermal growth factor receptor (EGFR) is a transmembrane protein that is a receptor for members of the EGF family of extracellular protein ligands. In many cancer types, mutations affecting EGFR expression or activity could result in cancer. Specifically, EGFR gene changes occurred in nearly 60% of glioblastoma tumors....

ASP4132 is an Orally Active AMPK Activator

Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is an enzyme that plays a role in cellular energy homeostasis. Specifically, it is important in largely to activate glucose and fatty acid uptake and oxidation when cellular energy is low. Besides, AMP or adenosine diphosphate (ADP) levels increase during metabolic stress such...

TNP-351, an Antifolate, is a Dihydrofolate Reductase (DHFR) Inhibitor

Antifolates are a class of antimetabolite medications that block the actions of folic acid. Antimalarial antifolates have been central for prophylaxis and treatment of malaria. The success of antifolates in the treatment of tumors also leads to the use of this class of drugs in the treatment of other...

XZ739 is a PROTAC BCL-XL Degrader

PROTAC is an emerging therapeutic modality. PROTAC is a feasible solution to reduce platelet toxicity associated with BCL-XL inhibition. BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance. As a result, BCL-XL is an attractive target for cancer treatment. Specifically, XZ739 is a CRBN-dependent BCL-XL degrader. XZ739,...