Tag: STAT3

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...

G5-7, an Orally Active JAK2 Inhibitor, Induces Cell Cycle Arrest and Apoptosis

JAK2 and STAT3 have been extensively implicated in the development and progression of numerous cancers. STAT3 be also activated by EGFR, JAK2, and other TYKs activated by EGF, LIF, and other cytokines. STAT3 constitutively activats in 60% of primary malignant gliomas, and the extent of activation correlates with glioma...

SC99 is an Orally Active and Selective STAT3 Inhibitor

STAT3 is a member of the STAT protein family. STAT3 mediates the expression of a variety of genes in response to cell stimulation. So it plays a key role in many cell processes, such as cell growth and apoptosis. Specifically, the oncogenic STAT3 signaling pathway is becoming a promising...