Brusatol (NSC 172924) is a Nrf2 Inhibitor
Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS). Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. Meanwhile, Nrf2 is a transcription factor that regulates cellular...
Rapamycin is a Specific mTOR Inhibitor
mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...
GGTI-2154 is a Selective Geranylgeranyltransferase I (GGTase I) Inhibitor
The Ras superfamily of low molecular weight GDP/GTP-binding GTPases is critical in the regulation of many important biological events. They include the cell division cycle, survival and death, differentiation, and development. These GTPases also show a relation with oncogenesis, Ras and Rho proteins mediate malignant transformation, invasion, and metastasis....
PTC-209 is a Specific BMI-1 Inhibitor and Impairs the Tumor Microenvironment
Glioblastoma multiforme (GBM) is the most common and aggressive brain tumor and refractory to existing therapies. BMI-1 is part of the polycomb repressive complex 1 (PRC1). There is a statistically significant correlation between the high frequency of BMI-1-positive tumor cells and poor prognosis of patients according to the data...
APS-2-79 is a KSR-Dependent Antagonist of RAF-Mediated MEK Phosphorylation
Deregulation of the Ras-MAPK pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Kinase suppressor of Ras (KSR) is a MAPK scaffold. KSR exhibits allosteric regulation through dimerization with RAF. In this study, researchers developed a class of compounds that...
IMT1 is a First-in-Class Specific and Noncompetitive Human POLRMT Inhibitor
Mitochondria provide cellular energy through its oxidative phosphorylation system, which needs to coordinate the expression of genes encoded by nuclear and mitochondrial genomes (mtDNA). Specifically, the transcription of mtDNA in circular mammals depends on a single mitochondrial RNA polymerase (POLRMT). Besides, three proteins are required for mitochondrial transcription initiation:...
CXD101 is a Selective and Orally Active Class I HDAC Inhibitor
Aberrant expression of classical HDACs associates with a variety of malignancies, including solid and hematological tumors. HDACs have also been found broadly dysregulated in multiple myeloma (MM). In particular, the mechanisms that HDACs regulate tumorigenesis are quite diverse. HDACs induce a range of cellular and molecular effects through the...