SB-332235 is an Orally Active CXCR2 Antagonist

Chemokines are low m.w. proteins that modulate the immune response through the chemoattraction and activation of leukocytes. These mediators have four classes. Chemokines in which the first two cysteines are separated by a  single,  nonconserved amino acid are CXC or chemokines, while those containing adjacent N-terminalcysteine residues are  CC ...

LYN-1604 is a Potent ULK1 Activator

UNC-51 like kinase 1 (ULK1) is the mammalian homolog of ATG1. ULK1 is an autophagic initiator that may decide the subsequent cell fate. In the autophagic process, ULK1 is a component of the ULK complex that is essential for autophagy induction in different types of cancer. Additionally, characterization of ULK1 expression...

MS049 is a Selective and Dual Inhibitor of PRMT4 and PRMT6

Protein arginine N-methyltransferase 4 (PRMT4) methylation of arginine residues in proteins plays a key role in transcriptional regulation. Specifically, PRMT4 binds to transcription activators called p160 and CBP/P300. Besides, the modified forms of these proteins are involved in the stimulation of gene expression through steroid hormone receptors. Moreover, PRMT4...

L-Moses Disrupts PCAF-Brd Histone H3.3 Interaction

Bromodomains proteins (Brds) bind to acetylated lysines (KAc) through the Brd acetyllysine-binding site. Misregulation of these proteins is linked to the onset and progression of multiple disease states. They include cancer, HIV infection, and neuroinflammation. The p300/CBP-associated factor, PCAF (KAT2B), is a multi-domain protein. It contains a single Brd,...

Miransertib is an Orally Active, Selective and Allosteric Akt Inhibitor

The AGC kinases AKT1, AKT2, and AKT3 are key mediators of the PI3K/AKT/mTOR signaling pathway. Additionally, AKT promotes diverse physiological processes, including cell proliferation, migration, and protein synthesis, et al. In this article, we will introduce an allosteric Akt inhibitor, Miransertib. As a potent inhibitor, Miransertib exhibits  IC50s of...

Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor

Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...

APS-2-79 is a KSR-Dependent Antagonist of RAF-Mediated MEK Phosphorylation

Deregulation of the Ras-MAPK pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Kinase suppressor of Ras (KSR) is a MAPK scaffold. KSR exhibits allosteric regulation through dimerization with RAF. In this study, researchers developed a class of compounds that...