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…
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…
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…
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…
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.…
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…
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…
LDN-192960 is a Dual Haspin and DYRK2 Inhibitor
Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis. This phosphorylation generates a binding site on H3 for Survivin. Thus, the positions the Chromosome Passenger Complex…
TH34, an HDAC6/8/10 Inhibitor, Induces Caspase-Dependent Programmed Cell Death
HDAC (Histone deacetylases) are a group of proteins that act on histones. They remove acetyl groups from N-acetyl lysine amino acid on a histone. As a result, histones wrap DNA…