AZD1208 is an Orally Bioavailable and Highly Selective PIM Kinases Inhibitor
Pim kinases, also known as serine/threonine kinases, have three highly homologous isoforms namely Pim-1, Pim-2, and Pim-3. And Pim-1, Pim-2, and Pim-3 are recurrent proviral integration locus in Moloney murine leukemia virus. The overexpression of Pim kinases occurs when viral inserts at this site. Pim kinases are overexpressed in...
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...
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...
UZH1a is a Selective METTL3 Inhibitor
METTL3/14 plays a critical role in disorders associated with abnormal self-renewal, aberrant proliferation, and blocking differentiation of hematopoietic cells. Both METTL3 and METTL14 are upregulated in all subtypes of AML, despite the heterogeneity of this blood cell cancer in terms of chromosomal rearrangement and gene mutations. AML and B-cell...
YUM70, a Selective GRP78 Inhibitor, Induces ER Stress-Induced Apoptosis
GRP78 (Glucose-regulated protein, 78 kDa) is a key regulator of endoplasmic reticulum (ER) stress signaling. In this study, researchers describe the discovery of a series of GRP78 inhibitors. YUM70 is an ER stress inducer and kills cells by activating the apoptosis pathway. Especially, YUM70 treatment induces ER stress and...
Conglobatin, an Orally Active Hsp90 Inhibitor, Disrupts Hsp90-Cdc37 Complex Formation
Heat shock protein (Hsp) 90 is a chaperone protein. In addition to protecting cells by correcting misfolded proteins, Hsp90 also plays a key role in regulating the stability, maturation, and activation of a wide range of client substrates, including kinases, hormone receptors, and transcription factors. Most Hsp90 client proteins,...
Z-LE(OMe)TD(OMe)-FMK is a Selective Caspase-8 Inhibitor
Cysteine proteases implicate in apoptosis and cytokine processing. Caspase-8 is a member of the cysteine proteases. In particular, Caspase-8 is the molecular switch for apoptosis, necroptosis and pyroptosis. Z-LE(OMe)TD(OMe)-FMK is a selective caspase-8 inhibitor. Besides, Z-LE(OMe)TD(OMe)-FMK shows its antiproliferative and cytotoxic activity via induction of apoptosis. Caspase-8 is the...