Category: Lymphoma

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...

TL13-12 is a Selective ALK-PROTAC Degrader

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase. ALK is an attractive target for cancer therapies not only for its prominent role in a number of malignancies but also for its scant expression in normal adult tissue. Therapeutic strategies that target ALK may provide ways to further delay...

Mepazine, an Apoptosis Enhancer, is a Potent and Selective MALT1 Inhibitor

Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), a positive regulator of NF-κB, is amongst the top highly induced genes. In lymphocytes, MALT1 regulates NF-κB signaling through a scaffold function that transduces signals from the CBM complex to TRAF6, which subsequently activates downstream signaling. As a paracaspase, MALT1 also...