Tag: STAT3

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...

SC-43 is a Potent and Orally Active SHP-1 Agonist and STAT3 Phosphorylation Inhibitor

Cholangiocarcinoma (CCA) is the second most common hepatic malignancy after hepatocellular carcinoma (HCC). CCAs are epithelial malignancies that arise from cholangiocytes and are aggressive behavior and advanced clinical stage. STAT3 belongs to a family of transcription factors that relay cytokine receptor-generated signals into the nucleus. STAT3 is activated by...

HJC0416 is a Highly Potent and Orally Active STAT3 Inhibitor

Signal transducer and activator of transcription 3 (STAT3) is involved in the regulation of early embryonic development, angiogenesis, immune response, cell proliferation, and apoptosis. Additionally, STAT3 overexpresses in many cancers. As a result, it becomes an attractive therapeutic target for various cancer treatment studies. However, despite much intensive researches...

SI-109, a STAT3 Transcription Inhibitor, is the Ligand of PROTAC Degrader SD-36

As we have written in the article “SD-36 is a Selective PROTAC STAT3 Degrader”, proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Longchuan Bai, et al have...