Tag: STAT5

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...

AC-4-130 is a Potent STAT5 SH2 Domain Inhibitor

Signal transducer and activator of transcription 5 (STAT5) is a member of the STAT protein family. It is relevant to cell growth and differentiation. Specifically, STAT5 protein has related to cytoplasmic signal transduction and mediates the expression of specific genes. Abnormal STAT5 activity is closely related to a variety...

Stafib-1 is the First Selective Inhibitor of the STAT5b SH2 Domain

The transcription factor STAT5A/B controls leukemic cell survival and disease progression. Especially, STAT5B as major STAT5 isoform driving BCR/ABL+ leukemia. Besides, STAT5B enables transformation by suppressing IFN-α/γ, thereby facilitating leukemogenesis. STAT5b might serve as an anticancer target in ductal pancreatic adenocarcinoma. Stafib-1 acts as the first selective inhibitor of...

SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader

Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...