Targapremir-210, a Selective miR-210 Inhibitor, Targets the Dicer Site in Pre-miR-210
Hypoxia is a non-physiological level of oxygen tension, a phenomenon common in a majority of malignant tumors. Hypoxia associates with tumor progression, resistance to therapy, and metastasis in cancer. Numerous pathways play critical roles in cancer maintenance, including noncoding RNAs such as microRNA (miR)-210 that regulates hypoxia-inducible factors. In...
GSK621 is a Specific AMPK Activator, Inducing Autophagy and Apoptosis
AMPK is an enzyme, which plays a role in cell energy homeostasis. It mainly activates glucose and fatty acid uptake and oxidation when the cell energy is low. Specifically, AMPK is a major regulator of cell metabolism, which can exert its carcinogenic or antitumor activities. Besides, the activation of...
GSK143 is an Orally Active and Highly Selective Spleen Tyrosine Kinase (SYK) Inhibitor
Tyrosine-protein kinase SYK is an enzyme which in humans is encoded by the SYK gene. Specifically, Syk is a 72 kDa cytoplasmic non-receptor tyrosine kinase and it is relevant to in a variety of signal transduction cell types. Besides, Syk and ZAP-70, which are related to the zeta chain,...
HLI373 is an Efficacious Hdm2 Inhibitor, with Antimalarial Activity
Hdm2 is an ubiquitin-protein ligase. Hdm2 suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. HLI373 is an efficacious Hdm2 inhibitor. HLI373 is effective in inducing apoptosis of several tumor cell lines that are sensitive to DNA-damaging agents. These results suggest that HLI373 could serve...
XMU-MP-3 is a Potent Non-Covalent BTK Inhibitor and Induces Apoptosis
BTK, a nonreceptor tyrosine kinase member of the Tec kinase family, plays a significant role in B-cell development. BTK is a unique therapeutic target in B-cell malignancies. XMU-MP-3, a noncovalent inhibitor with potent BTK inhibitory. XMU-MP-3 suppresses BTK kinase activity both in vitro and in vivo. In addition, XMU-MP-3...
DI-87 is an Orally Active and Selective Deoxycytidine Kinase (dCK) Inhibitor
Deoxyribonucleotide triphosphates (dNTPs) are essential for tumor growth, and DNA replication and repair also is essential dNTPs. Parallel and convergent de novo and salvage pathways redundantly produce the same dNTPs using different substrates. The de novo pathway produces dNTPs from glucose and amino acids and is dependent upon ribonucleotide reductase (RNR)....
RA-9 is a Selective Proteasome-Associated DUBs Inhibitor
The ubiquitin-proteasome-system (UPS) is responsible for most of the intracellular protein degradation in eukaryotes. UPS consists of three components: the proteasomes, the ubiquitin conjugating system, and the deubiquitinating enzymes (DUBs). DUBs deconjugate ubiquitin from targeted proteins and this step is essential for protein degradation. The de-ubiquitination is required for...