Month: November 2022

STF-31 is a Selective GLUT1 Inhibitor and Used for Efferocytosis Rearch

Glucose transporter 1 (or GLUT1), also known as SLC2A1), is a member of membrane transport proteins. GLUT1 facilitates the transport of glucose across the plasma membranes of mammalian cells. Low glucose levels can promote GLUT1 expression in cell membranes. GLUT1 is also a major receptor for the uptake of...

JS25, a Selective and Covalent BTK Inhibitor, Acts by Segregating Tyr551

BTK, Bruton’s tyrosine kinase, belongs to the cytoplasmatic kinases TEC subfamily. BTK involves in immune regulation, and is activated by Src kinases. Then BTK leads to phospholipase-Cγ (PLCγ) phosphorylation, Ca2+ mobilization, and NF-κB/MAP activation. Meanwhile, BTK increases proinflammatory cytokines IL-6 and IL-10 production and controls integrin-mediated B-cells adhesion. Moreover,...

Abexinostat is an Orally Available Pan-HDAC Inhibitor

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. To date, There are 18 human HDACs. Besides, HDACs include four classes on the basis of their homology with yeast proteins. Class I HDACs (HDAC1, 2, 3, and...

JBJ-09-063 is a Mutant-Selective Allosteric EGFR Inhibitor

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor. And the IC50 values are 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM for EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S, and EGFRLT/L747S, respectively. JBJ-09-063 is remarkably effective at inhibiting cell growth. And it also leads to a significant increase in apoptosis. JBJ-09-063 is effective...

STX-0119 is a Selective, Orally Active STAT3 Dimerization Inhibitor

STAT3 protein is a potential cytoplasmic transcription factor. Constitutive activation of signal transducer and activator of transcription 3 (STAT3) is related to the proliferation, survival, invasion, and angiogenesis of many human cancer cells. Specifically, it transmits signals of cytokines and growth factors from the cell membrane to the nucleus...

GN25 is a Specific p53-Snail Binding Inhibitor with Antitumor Effects

P53, also known as Tumor protein P53, or transformation-related protein 53 (TRP53) is a regulatory protein that is often mutated in human cancers. Besides, p53 is the strongest tumor suppressor gene. In addition, p53 also induces cell death, and growth arrest and suppresses metastasis in response to various kinds...

ABT-510 is an Anti-Angiogenic Thrombospondin Peptide

Angiogenesis is the growth of new capillaries from existing blood vessels. Steps toward angiogenesis include protease production, endothelial cell migration, and proliferation, vascular tube formation, anastomosis of newly formed tubes, synthesis of a new basement membrane, and incorporation of pericytes and smooth muscle cells. The process of angiogenesis is...