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TOPK

TOPK (T-lymphokine-activated killer cell–originated protein kinase, also known as PBK or PDZ-binding kinase) is a Ser/Thr protein kinase that is highly expressed in many types of human cancer, including breast and lung cancers. TOPK is included in the “consensus stemness ranking signature” gene list that is up-regulated in cancer stem cell-enriched tumors and is associated with poor prognosis in multiple types of cancer.

TOPK/PBK is an oncogenic kinase upregulated in most human cancers. TOPK is important for mitotic cell division and that phosphorylation by Cdk1 is needed for its activation.

TOPK, a member of the MEK3/6-related MAPKK family, is expressed in a wide range of proliferating cells and tissues, including cancer cells and testis. TOPK negatively regulates the activity of p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1. The MAPK phosphatase MKP1, an archetypal member of the MKP family, plays a pivotal role in the deactivation of p38 through a dephosphorylation reaction.

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  2. GC32181 Cefradine (Cephradine) Cefradine (Cephradine) (Cefradine) ist ein Breitspektrum- und oral aktives Cephalosporin. Cefradine (Cephradine)  Chemical Structure
  3. GC12201 HI TOPK 032 HI TOPK 032 ist ein potenter und spezifischer TOPK-Hemmer. HI TOPK 032  Chemical Structure
  4. GC60929 Ilaprazole sodium Ilaprazol (IY-81149) Natrium ist ein oral aktiver Protonenpumpenhemmer. Ilaprazole sodium  Chemical Structure
  5. GC12304 OTS514 OTS514 ist ein hochpotenter TOPK-Inhibitor mit einem IC50 von 2,6 nM. OTS514 unterdrÜckt stark das Wachstum von TOPK-positiven Krebszellen. OTS514 induziert Zellzyklusarrest und Apoptose. OTS514  Chemical Structure
  6. GC16511 OTS964 OTS964 ist ein oral aktiver, hochaffiner und selektiver TOPK-Inhibitor (T-lymphokin-activated killer cell-originated protein kinase) mit einem IC50 von 28 nM. OTS964 ist auch ein potenter Inhibitor der Cyclin-abhÄngigen Kinase CDK11, die mit einer Kd von 40 nM an CDK11B bindet. OTS964  Chemical Structure

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