W1131 is a Potent STAT3 Inhibitor for Gastric Cancer Research
STAT3 is a key oncogene whose overactivation leads to cancer. As a transcription factor, it exhibits dual functions of signal transduction and transcriptional activation. Gastric cancer is a malignant tumor usually inhibited by 5-FU chemotherapy. However, this therapy can easily lead to resistance of cells to 5-FU. Therefore, the researchers found...
MC0704 is a STAT3 Inhibitor for Triple-negative Breast Cancer Research
Breast cancer (BC) is one of the main causes of cancer-associated death in women. And, BC is high recurrence and/or metastatic potential. BC is typically categorized into respective subtypes based on the presence of representative receptors (the human epidermal growth factor receptor, estrogen receptor, and progesterone receptor). Hence, these...
HM43239 is an Orally Active and Selective FLT3 Inhibitor
Acute myeloid leukemia (AML) is the most common acute leukemia in adults, with an incidence of over 20 000 cases per year in the United States alone. Large chromosomal translocations, as well as mutations in the genes involved in hematopoietic proliferation and differentiation, result in the accumulation of poorly...
SD-1029 is a JAK2/STAT3 Activation Inhibitor
Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. JAK includes JAK1, JAK2, JAK3 and TYK2. JAK serves as the cytoplasmic signaling components of cytokine receptors and are activated through cytokine-mediated trans-phosphorylation. The pseudokinase domain of JAKs is crucial...
Ganetespib (STA-9090) is a HSP90 Inhibitor
Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...
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...
ENMD-1198, an Orally Active Tubulin-Binding Agent, Reduces HIF-1α and STAT3 Activity
Hepatocellular carcinoma (HCC) is the fifth most cancer worldwide, with a continuously increasing incidence. HCC represents a hyper vascularized tumor and its progression is closely related to angiogenesis. Hepatocellular carcinoma overexpresses the vascular endothelial growth factor (VEGF). The transcription factor HIF-1α also plays a central role in HCC progression...