Category: Colorectal Cancer

LY3177833 is an Orally Active CDC7 and pMCM2 Inhibitor

CDC7 is a serine/threonine kinase and plays an important role in the initiation of DNA replication. . In this article, we will introduce a potent CDC7 and pMCM2 inhibitor LY3177833. LY3177833 has an  IC50 of 3.3 nM against CDC7. Upregulation of CDC7 has been observed in numerous tumor cell...

Parsatuzumab (RG 7414) is a Humanized mAb, Binding to EGFL7

Epidermal Growth Factor like domain 7 (EGFL7) is an endothelial cell-derived factor, mostly expressed in endothelial cells. EGFL7 takes part in the regulation of the spatial arrangement of cells during vascular tube assembly. The Egfl7 gene encodes active miR-126 which is related to cardiovascular diseases as well as the...

AZ31 is a Highly Selective and Orally Active ATM Inhibitor

Ataxia telangiectasia mutated (ATM) is an ATP-dependent phosphatidylinositol 3-kinase-related kinase (PIKK) serine/threonine protein kinase. ATM is related to ATR, DNA-PKcs, mTOR, SMG1 and the non-enzymatic TRRAP within this enzyme family. Importantly, ATM is a central player in the mitotic DNA damage response (DDR), increasing the response to DNA double-strand...

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...