DK419 Is a Potent Inhibitor of Wnt/β-Catenin Signaling for Colorectal Cancer Treatment
Colorectal Cancer (bowel cancer; colon cancer) is one of the most serious cancer diseases, with the development from colon or rectum. It is mainly due to old age and environmental factors. Although we have discovered batches of anti-cancer agents, they are still lacking. Wnt/β-Catenin signaling is a canonical Wnt...
TAS4464, a Highly Potent and Selective Inhibitor of NEDD8 Activating Enzyme, Shows Antitumor Activity
TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, shows antitumor activity. NEDD8 activating enzyme (NAE) is an essential regulator of the NEDD8 conjugation pathway. The ubiquitin-like modifier NEDD8 controls the stability and activity of its target proteins via a conjugation cascade (the neddylation pathway). NAE controls...
AMG 487, a Selective CXCR3 Antagonist, Has Potential to Treat Metastatic Cancer
In previous blog, we introduced AMG 487 as a potent, orally active and selective CXCR3 antagonist, which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively. Today, I’d like to describe the antitumor effect of AMG 487 on metastatic cancer....
GW7604, the Metabolite of GW5638, is a Selective Estrogen Receptor Downregulator (SERD)
Drugs that inhibit estrogen receptor alpha (ERα) or which block the production of estrogens remain frontline interventions in the treatment and management of breast cancer at all stages. In this study, researchers found that molecular mechanism of action at estrogen receptor α of GW7604. GW7604 is a clinically relevant...
NG25, a Dual Inhibitor of TAK1 and MAP4K2, Enhances Doxorubicin-mediated Apoptosis in Breast Cancer
In previous blog, we described NG25 as a potent dual TAK1 and MAP4K2 inhibitor. The compound shows excellent inhibition for inhibiting IKKβ activation by TLR7 and TLR9 agonists. Today, I’d like to introduce the anti-tumor activity of NG25 in breast cancer. A study from Zhenyu Wang carried out a...
PTC299 is an Oral Active and Dual Inhibitor of DHODH and VEGF
De novo pyrimidine nucleotide biosynthesis is activated in proliferating cancer cells in response to an increased demand for synthesis of DNA, RNA and phospholipids. The synthesis activates via oncogenic pathways, such as Myc, PI3K, PTEN and mTOR. Dihydroorotate dehydrogenase (DHODH) locates on the surface of the inner mitochondrial membrane,...
MA242 is a Dual Inhibitor of MDM2 and NFAT1
Overexpression and activation of the murine double minute 2 (MDM2) or nuclear factor of activated T cells 1 (NFAT1) oncoproteins occur frequently in pancreatic cancer. Many MDM2 inhibitors target MDM2-p53 binding and have little or no effect on cancers without functional p53, such as pancreatic cancer. Besides, nuclear factor...