TOPK

OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM.

OTS514, a thieno[2,3-c]quinolone compound, is a highly potent TOPK inhibitor with an IC50 value of 2.6 nM. The compound can inhibit TOPK kinase activity.

HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities.

Cephradine monohydrate (Cefradine monohydrate) is a first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria.

OTS964 is a selective inhibitor of T-cell orientation protein kinase (TOPK), demonstrating a high affinity with an IC50 of 28 nM. Additionally, OTS964 effectively inhibits cyclin-dependent kinase 11 (CDK11), with a binding affinity (Kd) of 40 nM for CDK11B. This compound is utilized in research exploring cancer therapeutic strategies and cell cycle regulation.

SKLB-C05 is a highly selective, orally active inhibitor of the T-Lymphokine-Activated Killer Cell-originated Protein Kinase (TOPK), exhibiting an IC50 of 0.5 nM. This compound has demonstrated the ability to induce apoptosis, downregulate c-Myc, and activate p53 while disrupting FAK/Src-mediated migratory signaling. Additionally, SKLB-C05 interferes with cell mitosis and displays significant anticancer activity specifically against TOPK-positive colorectal cancer, making it a valuable tool for cancer research.

TOPK-p38/JNK-IN-1 is an orally active inhibitor targeting the TOPK-p38/JNK signaling pathway, exhibiting an IC50 value of 2.14 µM for nitric oxide production. This compound demonstrates significant anti-inflammatory activity by inhibiting the phosphorylation of downstream proteins while preventing degradation of TOPK. Research applications include studies on inflammatory processes and cellular signaling mechanisms in various disease models.