BPDA2 is a Highly Selective and Competitive SHP2 Inhibitor
SH2-containing protein tyrosine phosphatase 2 (SHP2) is a carcinogenic phosphatase. Specifically, SHP2 participates in the downstream signal transmission of various RTK. So it is the shared signal node for analysis. The phosphatase activity of SHP2 is necessary for important cancer-related signaling pathways (such as RAS and PI3K). Besides, the...
FPDT is an anti-glioblastoma agent and shows anti-glioblastoma activity by AKT pathway.
FPDT (2-(4-fluorophenyloamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is an anti-glioblastoma agent. FPDT displays cytotoxic with IC50 values of 44-68 μM for GBM cells and >100 μM for human astrocytes HA. Besides, Anti-glioblastoma activity of FPDT is linked to downregulation of the AKT pathway. FPDT (0-100 µM; 48 h) shows anti-proliferative activity with IC50 values of 53.53, 44.98, 55.20, 56.37, 67.73, >100...
MS170 is a PROTAC AKT Degrader
The alternative name of serine/threonine kinase AKT is protein kinase B (PKB). Three closely related genes in humans: AKT1 (PKB-α), AKT2 (PKB-β), and AKT3 (PKB-γ) encode PKB. AKT is an important component of the PI3K/AKT/mammalian target of rapamycin (m-TOR) signaling pathway. It also regulates fundamental cellular and physiological processes,...
Deguelin, a Naturally Occurring Rotenoid, Acts as a Chemopreventive Agent
Head and neck squamous cell carcinoma (HNSCC) represents more than 5% of all cancers each year. In addition, breast cancer is a heterogeneous group of diseases. Approximately 60-70% of breast cancers express estrogen receptors (ER) and/or progesterone receptors (PR). About 20-30% of breast cancers have amplified levels of the...
Capivasertib (AZD5363) is an Orally Active pan-AKT Kinase Inhibitor
Akt/PKB (Protein kinase B), usually called Akt, is a serine/threonine protein kinase with antiapoptotic activity. In addition, Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis. Akt possesses a protein...
Golvatinib (E-7050) is a potent Dual Inhibitor of both c-Met and VEGFR2 Kinases
c-Met is the cellular receptor for the hepatocyte growth factor (HGF). Activation of the HGF⁄c-Met pathway always leads to tumor progression, invasion, and metastasis. Vascular endothelial growth factor (VEGF) is an important molecule in tumor progression. Additionally, VEGF is associated with tumor angiogenesis. Due to their important role in...
Miransertib is an Orally Active, Selective and Allosteric Akt Inhibitor
The AGC kinases AKT1, AKT2, and AKT3 are key mediators of the PI3K/AKT/mTOR signaling pathway. Additionally, AKT promotes diverse physiological processes, including cell proliferation, migration, and protein synthesis, et al. In this article, we will introduce an allosteric Akt inhibitor, Miransertib. As a potent inhibitor, Miransertib exhibits IC50s of...