Category: Cancer

CID44216842 is a Potent Cdc42-Selective Guanine Nucleotide Binding Lead Inhibitor

Cdc42, a small GTPase of the Rho family, plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal disorders. Therefore, Cdc42 inhibitors will be useful in probing molecular pathways and could...

PD-089828 is an Inhibitor of FGFR-1, PDGFR-β, EGFR and c-Src Tyrosine Kinase

Protein tyrosine kinases comprise a group of enzymes. They catalyze the phosphorylation of certain proteins on specific tyrosine residues. The growth factor receptor tyrosine kinases are a subfamily. The kinases are activated on the high-affinity binding of growth factors to their cognate receptors. Members of this subfamily include PDGFR...

HSD1590 is Potent ROCK Inhibitor with Low Cell Toxicity

Rho-associated protein kinases (ROCKs) are serine-threonine kinases contain isoforms ROCK1 and ROCK2. ROCK1 and ROCK2 exhibit 60% sequence homology and 90% kinase domain homology. The 2 isoforms exist in many organs/tissues but have different expression levels. ROCK1 mainly expresses in thymus, tongue, spleen, and cervix, et al. ROCK2 exists...

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...

SB-633825 is a Potent Inhibitor of TIE2, LOK (STK10) and BRK

Protein kinase is a kind of kinase and can modify other proteins (phosphorylation) by adding other phosphorylation groups. Specifically, phosphorylation usually changes the function of target protein (substrate) by changing enzyme activity, cell location, or association with other proteins. Besides, protein kinases have become a rich source of drug...

iFSP1 is a Selective FSP1 Inhibitor Glutathione-Independently

Ferroptosis is an iron-dependent form of necrotic cell death marked by oxidative damage to phospholipids. Selenoenzyme GPX4 could control Ferroptosis. Flavoprotein apoptosis-inducing factor mitochondria-associated 2 (AIFM2) is an anti-ferroptosis gene. AIFM2 (ferroptosis suppressor protein 1, FSP1) confers protection against ferroptosis elicited by GPX4 deletion. The anti-ferroptosis function of FSP1...

DC-5163, a GAPDH Inhibitor, Inhibits Glycolysis Pathway and Induces Apoptosis

Cancer cells always exhibit abnormal energy metabolism. Abnormal energy metabolism often leads to an increase in glucose uptake and lactic acid fermentation. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) is an important catalyzing enzyme for glycolysis. GAPDH catalyzes key steps at the center of the glycolysis process. And this process is the convergence...