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.

Targets for TOPK

Products for TOPK

Cat.No. Nombre del producto Información
GC32181 Cefradine (Cephradine) Cefradine (Cephradine) (Cefradine) es una cefalosporina de amplio espectro y activa por vÍa oral.
GC12201 HI TOPK 032 HI TOPK 032 es un potente y específico inhibidor de TOPK.
GC60929 Ilaprazole sodium El ilaprazol (IY-81149) sÓdico es un inhibidor de la bomba de protones activo por vÍa oral.
GC12304 OTS514 OTS514 es un inhibidor de TOPK muy potente con una IC50 de 2,6 nM. OTS514 suprime fuertemente el crecimiento de células cancerosas positivas para TOPK. OTS514 induce la detenciÓn del ciclo celular y la apoptosis.
GC16511 OTS964 OTS964 es un inhibidor de TOPK (proteÍna quinasa originada en células asesinas activada por linfocina T) activo por vÍa oral, de alta afinidad y selectivo con una IC50 de 28 nM. OTS964 también es un potente inhibidor de la cinasa dependiente de ciclina CDK11, que se une a CDK11B con una Kd de 40 nM.