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.

対象は TOPK

製品は TOPK

Cat.No. 商品名 インフォメーション
GC32181 Cefradine (Cephradine) セフラジン（Cephradine）（Cefradine）は、広域スペクトルで経口的に活性なセファロスポリンです。
GC12201 HI TOPK 032 HI TOPK 032 は、強力で特異的な TOPK 阻害剤です。
GC60929 Ilaprazole sodium イラプラゾール (IY-81149) ナトリウムは、経口活性プロトンポンプ阻害剤です。
GC12304 OTS514 OTS514 は、IC50 が 2.6 nM の非常に強力な TOPK 阻害剤です。 OTS514 は、TOPK 陽性のがん細胞の増殖を強力に抑制します。 OTS514 は、細胞周期の停止とアポトーシスを誘導します。
GC16511 OTS964 OTS964 は、28 nM の IC50 を持つ、経口活性、高親和性、選択的 TOPK (T-リンフォカイン活性化キラー細胞由来プロテインキナーゼ) 阻害剤です。 OTS964 はサイクリン依存性キナーゼ CDK11 の強力な阻害剤でもあり、40 nM の Kd で CDK11B に結合します。