Category: Melanoma

MYLS22 is a Selective Optic Atrophy 1 (OPA1) Inhibitor

Optic neuropathy is damage to the optic nerve from any cause. Specifically, damage and death of these nerve cells, or neurons, leads to characteristic features of optic neuropathy. Angiogenesis requires an internal mitochondrial membrane mitochondrial fusion protein optic atrophy 1 (OPA1). Besides, mitochondrion fusion is controlled by mitochondrion fusion...

BAY-985 is an Orally Active and ATP-Competitive TBK1/IKKε Inhibitor

The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homolog IKKε plays an important role in cellular pathways. And, as we all know, these kinases belong to the nuclear factor κB family. In this article, we will introduce a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε,...

IACS-8803 is a Cyclic Dinucleotide STING Agonist

The stimulator of interferon genes (STING) is an innate pattern recognition receptor natively exists in the endoplasmic reticulum (ER). STING has a great effect on host defense through supervising pathogenic or damage-associated nucleic acids. Since the generation of optimal adaptive anti-tumor immune responses requires the STING signal, activation of...

CCG-222740 is a Selective Rho/MRTF Pathway Inhibitor

Pancreatic cancer is one of the most lethal cancers, is characterized by a strong fibro-inflammatory reaction composed mainly of cancer-associated fibroblasts. Pancreatic stellate cells (PSCs) present in the pancreas tumor microenvironment. PSCs can excrete essential amino acids and cytokines to maintain an immunosuppressive environment. CCG-222740 is a potent and...

Tasisulam, an Antitumor Agent, Inhibits Mitotic Progression and Induces Apoptosis

Tasisulam is an acyl sulfonamide with a unique antitumor dual mechanism of action. It involves antiangiogenesis and mitotic inhibition. Tasisulam has a broad range of activity in 60 tumor cell lines. It includes leukemia, melanoma, non-small-cell lung cancer, colon, ovarian, renal, and breast cancers. In this study, Tasisulam is...

Ravoxertinib is an Orally Active and Highly Selective ERK1/2 Inhibitor

The RAS/RAF/MEK/ERK (MAPK) signal transduction pathway has attracted significant interest as a therapeutic target for cancer. ERK1/2 phosphorylates more than 50 downstream substrates responsible for cell growth, proliferation, survival, angiogenesis, and differentiation. Small molecule inhibitors of BRAF and MEK have shown promising activities in a variety of solid tumors...