Category: Glioma

A-674563 is an Orally Active and Selective Akt1 Inhibitor

Akt1 belongs to the Akt subfamily of serine/threonine kinases, which contains the SH2 (SRC homologous 2-like) domain. Specifically, Akt kinase is the central node of the signal transduction pathway, which is important for cell transformation and tumor progression. Besides, Akt is a key mediator of growth factor-induced neuronal survival...

BIM-23190 is a Selective SSTR2 and SSTR5 Agonist

Somatostatin (SST) is a peptide hormone, which can regulate the endocrine system. Specifically, Somatostatin affects neurotransmission and cell proliferation by interacting with G protein-coupled somatostatin receptors and inhibiting multiple releases. Besides, Somatostatin inhibits insulin and glucagon secretion. Moreover, Somatostatin is produced by neuroendocrine neurons in the hypothalamic extraperitoneal nucleus....

AKI603 is an Aurora Kinase A Inhibitor with Anti-tumor Activity

Chemoresistance is a major cause of cancer treatment failure. Tumor-initiating cells (TIC) have attracted a considerable amount of attention due to their role in chemoresistance and tumor recurrence. The inhibition of AurA kinase by AKI603 abrogates the epirubicin-induced enrichment of TICs.In this study, researchers evaluated the small molecule Aurora...

G5-7, an Orally Active JAK2 Inhibitor, Induces Cell Cycle Arrest and Apoptosis

JAK2 and STAT3 have been extensively implicated in the development and progression of numerous cancers. STAT3 be also activated by EGFR, JAK2, and other TYKs activated by EGF, LIF, and other cytokines. STAT3 constitutively activats in 60% of primary malignant gliomas, and the extent of activation correlates with glioma...

M2698 is an Orally Active, ATP-Competitive, Selective, Dual p70S6K and Akt Inhibitor

The disorder of PI3K/Akt/mTOR (PAM) signaling pathway occurs in about 30% of human cancers, making it a reasonable target for new therapies. Specifically, the pathway is an important regulator of growth, proliferation, and metabolism. However, some PAM pathway inhibitors, such as Rapamycin complex (mTORC) rapalogs, cause the impairment of...

PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket

Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...

MN58b is a Selective Choline Kinase α Inhibitor

Choline kinase (CHK) catalyzes the phosphorylation of choline by ATP in the presence of Mg2+, yielding phosphocholine. This enzyme step commits choline to the Kennedy pathway for the biosynthesis of phosphatidylcholine, the major phospholipid constituent in biomembranes. Phosphatidylcholine has an essential structural function as well as serving as a...