PDZ-binding kinase, also known as PBK or T lymphokine-activated killer cell-originated protein kinase (TOPK), is a Ser/Thr protein kinase that is highly expressed in a variety of human cancers, including breast and lung cancers. The "consensus stemness ranking signature" gene list, which is up-regulated in tumors that are enriched in cancer stem cells and is linked to a poor prognosis in a number of cancer types, includes TOPK.

A common oncogenic kinase that is upregulated in most human cancers is TOPK/PBK. The activation of TOPK requires its phosphorylation by Cdk1, which is necessary for mitotic cell division.

TOPK, a member of the MAPKK family that is related to MEK3/6 and is found in a variety of proliferating cells and tissues, including testicles and cancer cells, is expressed. By phosphorylating the p38-specific phosphatase MKP1 and increasing its stability, TOPK inhibits the activity of p38. The MKP family's prototypical member, the MAPK phosphatase MKP1, is essential for the dephosphorylation reaction that results in the deactivation of p38.

TOPK related products

Structure Cat No. Product Name CAS No. Product Description
V22207 HI-TOPK-032 487020-03-1 HI-TOPK-032 is a novel, potent and selective TOPK kinase inhibitor which strongly suppressed TOPK kinase activity in vitro but had little effect on extracellular signal–regulated kinase 1 (ERK1), c-jun—NH2—kinase 1, or p38 kinase activities.
V3180 OTS514 1338540-63-8 OTS514 (OTS-514) is a novel TOPK (T-LAK cell-originated protein kinase) inhibitor with potential anticancer activity.
V2714 OTS514 HCl 2319647-76-0 OTS514 HCl (OTS 514; OTS-514), the hydrochloride salt of OTS514, is a novel and highly potent inhibitor of the TOPK (T-LAK cell-originated protein kinase) with potential antineoplastic activity.
V2721 OTS964 1338542-14-5 OTS964, a dimethylated derivative ofOTS514, is a novel and selectiveTOPK ((T-lymphokine-activated killer cell-originated protein kinase) inhibitor with potential anticancer activity.
V3181 OTS964 HCl 1338545-07-5 OTS964 HCl, the hydrochloride salt of OTS-964 and a dimethylated derivative of OTS 514, is a potent and selective inhibitor of TOPK (T-lymphokine-activated killer cell-originated protein kinase) with antitumor effects.
V55244 PBK-IN-9 1338540-55-8
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