Tag: Anti-Inflammatory

GPP78 is a Nampt Inhibitor and an Autophagy Inducer

Nicotinamide phosphoribosyltransferase (NAMPT) is an enzyme that catalyzes the synthesis of nicotinamide mononucleotide (NMN) from nicotinamide (NM) and PRPP. Therefore, NAMPT plays an important role in the cyclic biosynthetic pathway of nicotinamide adenine dinucleotide (NAD). Especially, NAMPT acts as an extracellular proinflammatory cytokine, able to induce cellular expression of...

CG-200745, a HDAC Inhibitor, Induces the Accumulation of p53

Histone deacetylase (HDAC) inhibits are considered to be promising agents that can be used as treatments for cancer. CG-200745 is a novel and potent hydroxamate-based pan-HDAC inhibitor. CG-200745 has the hydroxamic acid moiety to bind zinc at the bottom of the catalytic pocket. We will introduce its anti-tumorigenic property...

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...

MSX-122, a Partial Antagonist of CXCR4, Has Anti-Metastasis Activity

In previous blog “MSX-122 is a Partial Antagonist of CXCR4”, I described MSX-122 as an orally available, specific small molecule antagonist of CXCR4/CXCL12. And it has good anti-inflammatory properties. However, MSX-122 entered into clinical trials tested among breast cancer patients. Accordingly, MSX-122 is a promising clinical candidate for cancer...