SZUH280 is a Potent And Selective PROTAC HDAC8 Degrader
Histone deacetylase 8 (HDAC8) is a class I histone deacetylase. Unlike other class I HDACs, it localizes both in the nucleus and in the cytoplasm. HDAC8 can also target non-histone proteins, such as the structural maintenance of chromosome 3 (SMC3) cohesin protein, retinoic acid induced 1 (RAI1) and p53....
VAL-083 Creates DNA N7 Methylation with Antitumor Activity
Glioblastoma (GBM) is one of the most difficult tumors. Many new agents fail to cross the blood-brain barrier (BBB) and it has intrinsic drug resistance. VAL-083 is an alkylating agent that creates N7 methylation on DNA. Additionally, VAL-083 suppresses U251 and SF188 cell growth and induces apoptosis after 72...
Zingerone, an Orally Active Nontoxic Methoxyphenol, Possesses Anti-Inflammatory and Anti-Tumor Properties
Humans have been using natural products for medicinal use for ages. Ginger (Zingiber officinale) is used as a condiment worldwide from times immemorial. Ginger has many health benefits in traditional medicine. It is due to diverse phytochemical constituents present in ginger which lead to promising health benefits. It is...
MYCMI-6 is a Selective Endogenous MYC:MAX Inhibitor
The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables the MYC:MAX complex to bind E-box regulatory DNA elements throughout the genome. Therefore, it controls the transcription of a...
AKOS-22, a VDAC1 Oligomerization and Apoptosis Inhibitor, Protects Against Mitochondrial Dysfunction
Apoptosis plays a critical role in several pathological processes, such as neurodegenerative diseases and various cardiovascular diseases. Besides, it is therefore not surprising that mitochondrial dysfunction is associated with various human diseases. Located at the outer mitochondrial membrane (OMM), 2 the voltage-dependent anion channel (VDAC) serves as a mitochondrial gatekeeper. Moreover, the...
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...
JTE-013 is a Specific S1P2 Antagonist in Neuroblastoma
Sphingosine-1-phosphate ( S1P ), the bioactive sphingolipid metabolite, is a critical regulator of many physiological and pathophysiological processes, including cancer, atherosclerosis, diabetes and osteoporosis. S1P and its receptors (S1P1-5) play critical roles in many pathologic processes, including cancer. S1P/sphingosine-1-phosphate receptor (S1PR) axis plays critical role in a wide variety...