Tag: Anti-Inflammatory

IV-361 is an Orally Active and Selective CDK7 Inhibitor

Cyclin-dependent kinase 7 (CDK7) is a catalytic subunit of CDK activated kinase (CAK). CAK is a kinase complex that catalyzes T-ring phosphorylation and activates a variety of cyclin-related kinases, including CDK1, CDK2, CDK4, and CDK6. Importantly, CDK7 plays a role at the direct interface between important processes of cell...

Lumiracoxib is a Selective and Orally Active COX-2 Inhibitor and Nonselective NSAID

Prostaglandins play an important role in modulating both physiological and inflammatory processes. They can act as autocrine factors regulating platelet aggregation, vascular tone, and secretions. Additionally, the synthesis of prostaglandin depends on the activity of cyclooxygenase (COX). There are existing two isoforms: COX-1 and COX-2. They are highly homologous...

SB-332235 is an Orally Active CXCR2 Antagonist

Chemokines are low m.w. proteins that modulate the immune response through the chemoattraction and activation of leukocytes. These mediators have four classes. Chemokines in which the first two cysteines are separated by a  single,  nonconserved amino acid are CXC or chemokines, while those containing adjacent N-terminalcysteine residues are  CC ...

SP-8356 is a Potent and Orally Active CD147 Inhibitor

Breast cancer is one of the most fatal diseases in women and exhibits high incidence and mortality among various cancers. Among various signaling pathways that promote tumor growth and progression, an inflammatory transcription factor NF-κB plays pivotal roles on cell proliferation and survival. Interestingly, NF-κB is highly activated in...

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...