Category: Colorectal Cancer

CQ211 is a Potent and Selective RIOK2 Inhibitor

RIOK2 is a typical kinase implicated in multiple human cancers. The right open reading frame (RIO) kinases belong to the atypical kinases family. RIO kinases contain a C-terminal RIO domain that is structurally homologous to typical protein kinases. However, RIOKs lack the key motifs which can convert the enzyme from...

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Bestatin is a Broad-Spectrum, and Competitive Aminopeptidase Inhibitor

Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein or peptide substrates. Regarding catalytic mechanism, most of the aminopeptidases are metallo-enzymes. In addition, aminopeptidase is widely present in animal and plant kingdomsis widely present in , found in many subcellular organelles, in cytoplasm, and as...

ML-00253764 is a Brain Penetrant Melanocortin Receptor 4 Antagonist

The involuntary weight loss that occurs as some diseases poses a serious medical problem. For example, sarcopenia, cancer cachexia, rheumatoid arthritis, and hip fractures can lead to involuntary weight loss. The melanocortin 4 receptor (MC4R) plays a key role in body weight regulation and energy homeostasis. The signaling of...

Tetrac is a Thyrointegrin Receptor Antagonist

In the angiogenesis process, integrins are members of a family of cell surface transmembrane receptors. They play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as T4 and T3 promote angiogenesis and tumor cell proliferation via integrin αvβ3...

FR 180204 is an ATP-competitive and Selective ERK Inhibitor

An extracellular signal-regulated kinase (ERK) is a serine/threonine-protein kinase of the mitogen-activated protein kinase superfamily. Selective inhibition of ERK represents a potential approach for the treatment of cancer and other diseases. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

BI-882370 is a Novel Orally Active RAF Kinase Inhibitor

Cancers arise owing to the accumulation of mutations in critical genes that alter normal programmes of cell proliferation, differentiation and death. The RAS–RAF–MEK–ERK–MAP kinase pathway mediates cellular responses to growth signals. Three RAF genes code for cytoplasmic serine/threonine kinases. Whereas mutations in ARAF and CRAF are very rare, BRAF...