Category: Melanoma

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...

Birinapant (TL32711), a Bivalent Smac Mimetic, is an Antagonist for XIAP and cIAP1

XIAP is a protein that prevents apoptosis. XIAP is a member of apoptosis protein family (IAP) inhibitors. Specifically, IAP blocks cell death in vitro and in vivo by inhibiting different caspases. The caspase inhibitory activity of XIAP is negatively regulated by at least two XIAP interacting proteins XAF1 and...

AA92593 is a Selective and Competitive OPN4 (Melanopsin) Antagonist

Melanopsin (OPN4) is a photopigment in a small part of intrinsically photosensitive ganglion cells (ipRGC) of the mammalian retina. Meanwhile, Melanopsin is a photosensitive pigment, which is encoded by the OPN4 gene. Mutations in the OPN4 gene can lead to clinical diseases, such as seasonal affective disorder (SAD). Nonetheless,...

Piclidenoson is a First-in-Class and Orally Active A3AR Agonist

One of the main strategies for cancer research is the identification of drugs that can cause apoptotic death in malignant cells. Additionally, Adenosine 5′-triphosphate (ATP), UTP, and adenosine are considered that inhibit the growth of several cancerous cell lines. Adenosine has several physiological and pharmacological functions. It can modulate...

ML786 is an Orally Bioavailable Raf Inhibitor

The mitogen-activated protein kinase (MAPK) signal pathway plays an important role in cells. It also has a response to many different external stimuli and regulates cellular growth, proliferation. The Raf isoform B-Raf is one component of this pathway. Besides, it has a high rate of activating mutation in melanoma...

NHWD-870 is an Orally Active and Selective BET Bromodomain Inhibitor

Brominedomain can recognize acetylated lysine residues. As the “reader” of lysine acetylation, the bromine domain is responsible for the transduction of signals carried by acetylated lysine residues and transforming them into various normal or abnormal phenotypes. Specifically, the bromine domain-containing proteins have a variety of functions. Besides, it ranges...