Category: Lymphoma

CXD101 is a Selective and Orally Active Class I HDAC Inhibitor

Aberrant expression of classical HDACs associates with a variety of malignancies, including solid and hematological tumors. HDACs have also been found broadly dysregulated in multiple myeloma (MM). In particular, the mechanisms that HDACs regulate tumorigenesis are quite diverse. HDACs induce a range of cellular and molecular effects through the...

JH-XI-10-02 is a Highly Potent and Selective PROTAC CDK8 Degrader

PROteolysis Targeting Chimeras (PROTACs) regulate protein function by degrading target proteins instead of inhibiting them, providing more sensitivity to drug-resistant targets. PROTACs show better selectivity compared to classic inhibitors. PRTOACs have outperformed not only in cancer diseases but also in immune disorders, viral infections, and neurodegenerative diseases. PROTACs present...

CJ-2360 is a Potent and Orally Active ALK Inhibitor

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor (IR) kinase superfamily. It highly expresses in adult brain tissue and exerts an important role in the development of the nervous system. Deregulation of ALK originally presents by the identification of at (2;5) chromosomal translocation...

BI-3802-Induced Polymerization Triggers Degradation of BCL6

PROTAC has been developed to degrade a wide range of clinically relevant targets. These small-molecule degraders engage both the E3 ligase and the target protein to promote the formation of a substrate–drug–ligase ternary complex. Although degraders can show notable efficacy and sustained depletion of targets, some proteins are resistant....

CC-90010 is a Reversible and Orally Active BET Inhibitor

Come straight to the point, CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. The bromodomain and extra-terminal domain (BET) proteins, epigenetic readers, recognize and bind acetylated lysine residues. The BET protein family comprises the ubiquitously expressed...

UNC6852 is a Selective Rolycomb Repressive Complex 2 (PRC2) PROTAC Degrader

Polycomb repressive complex 2 (PRC2) is a multicomponent complex with histone methyltransferase (HMT) activity. H3K27 trimethylation (H3K27me3) is a key mechanism responsible for gene repression. In this study, researchers report the discovery of an EED-targeted bivalent chemical degrader. Researchers show that UNC6852 potently binds EED in vitro, degrades EED...

E7820 is an α2 Integrin Inhibitor with Anti-Tumor Activity

Vascular endothelial growth factor (VEGF) is a prime contributor to tumor angiogenesis. Most tumor cells produce high levels of VEGF and VEGF receptors associated with tumor endothelial cells. E7820 is an aromatic sulfonamide derivative and an Angiogenesis inhibitor. E7820 inhibits in vitro proliferation and tube formation of human umbilical...