Category: Colon Cancer

SZUH280 is a Potent And Selective PROTAC HDAC8 Degrader

Histone deacetylase 8 (HDAC8) is a class I histone deacetylase. Unlike other class I HDACs, it localizes both in the nucleus and in the cytoplasm. HDAC8 can also target non-histone proteins, such as the structural maintenance of chromosome 3 (SMC3) cohesin protein, retinoic acid induced 1 (RAI1) and p53....

Ganitumab (AMG 479) is an IGF1R mAb for Cancer Research

Insulin-like growth factor 1 (IGF-1) receptor is a transmembrane receptor. Specifically, it belongs to a large class of tyrosine kinase receptors. This receptor mediates the action of IGF-1, a polypeptide protein hormone with a molecular structure similar to insulin. Besides, IGF-1 plays an important role in the growth and...

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...

BSP16 is an Orally Active Stimulator of Interferon Genes (STING)

Interferon gene stimulator(STING) is an adaptor protein that can induce the secretion of type I interferon and proinflammatory cytokines. Meanwhile, the protein is activated by bacterial-derived cyclic dinucleotide (CDN) or cytosolic dsDNA (dsDNA). Downstream effects of STING activation include NF-κB. Nonetheless, IRF3 and STAT6 are active. This leads to...

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...