Category: Lymphoma

DM-01 is a Powerful and Selective EZH2 Inhibitor

Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and a...

GSK778 is a Potent and Selective Inhibitor of BET BD1

The bromodomain is a protein domain of about 110 amino acids, which can recognize acetylated lysine residues. Specifically, the bet (Bromo- and terminal domain) family consists of germ cell-specific (BRDT) and ubiquitously expressed (BRD2, BRD3, Brd4) epigenetic reader proteins. As a “reader” of lysine acetylation, bromodomain is responsible for...

XMU-MP-3 is a Potent Non-Covalent BTK Inhibitor and Induces Apoptosis

BTK, a nonreceptor tyrosine kinase member of the Tec kinase family, plays a significant role in B-cell development. BTK is a unique therapeutic target in B-cell malignancies. XMU-MP-3, a noncovalent inhibitor with potent BTK inhibitory. XMU-MP-3 suppresses BTK kinase activity both in vitro and in vivo. In addition, XMU-MP-3...

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...

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...

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,...

Zotatifin is a Selective and Well-Tolerated eIF4A (Protein Biogenesis) Inhibitor

In this article, we will introduce a potent, selective, and well-tolerated eIF4A inhibitor, Zotatifin. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM). Zotatifin is able to induce the formation of a stable ternary complex [eIF4A-RNA-eFT226]. Additionally, it increases the residence time for...