Tag: SRC

DGY-06-116 is an Irreversible Covalent and Selective Src Inhibitor

Src kinase family is a family of non-receptor tyrosine kinases. DGY-06-116 is a selective Src inhibitor. DGY-06-116 is an SRC-directed covalent kinase inhibitor that displays efficient covalent target labeling and irreversible cellular inhibition of SRC signaling. Furthermore, DGY-06-116 inhibits SRC for an extended duration, likely due to its ability...

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...

A 419259 is a Potent Src Inhibitor

Chronic myelogenous leukemia (CML) is a human malignancy and affects hematopoietic progenitor cells. The CML is driven by Bcr-Abl. Additionally, Bcr-Abl is a 210 kDa chimeric tyrosine kinase that transforms fibroblasts, growth factor-dependent hematopoietic cell lines. Bcr-Abl is a constitutively active protein-tyrosine kinase and can stimulate the proliferation and...

SM1-71 is a Multi-Targeted Kinase Inhibitor with Anti-Cancer Activity

In this article, we will introduce a potent TAK1 inhibitor, with a Ki of 160 nM. SM1-71 inhibits MEK1 activities with an IC50 of 142 nM. It also exhibits only weak activity against ERK2 with an IC50 of 1090 nM. Additionally, SM1-71 has an acrylamide warhead in the ortho-position. At the same time, it...

CGP77675 is an Orally Active Inhibitor of Src Family Kinases

Src kinase family is a nonreceptor tyrosine kinase family. It includs 9 members: SRC, yes, Fyn and FGR, Lck, HCK, BLK, and Lyn. Specifically, Src family kinases interact with many cytoplasmic, nuclear, and membrane proteins and modify these proteins by phosphorylation of tyrosine residues. Besides, tyrosine kinase SRC is...

AZD0424 is an Orally Active and Dual Selective Src/Abl Kinase Inhibitor

A study from Victoria K Woodcock suggested that AZD0424 is an inhibitor of the proto-oncogenic non-receptor tyrosine kinases Src and ABL1. The kinase plays an indefensible role in cancer. Src expresses lowly in the majority of cell types and participates in regulating bone metabolism, proliferation, and angiogenesis. Src also...

TL02-59 is a Selective and Orally Active Myeloid Src-family Kinase Fgr Inhibitor

Acute myelogenous leukemia (AML) is a devastating hematologic cancer with limited treatments. Scientists have demonstrated that diverse genetic changes are associated with AML. Especially, the upregulation of tyrosine kinase signaling pathways stands for a common feature. Additionally, mutations in the Flt3 receptor tyrosine kinase accounts for almost one-third of...