topk

HI-TOPK-032 is an effective and specific inhibitor of TOPK.

Ilaprazole (IY-81149) is a proton pump inhibitor used in the treatment of dyspepsia gastroesophageal reflux disease (GORD GERD) and duodenal ulcer. Studies also showed that Ilaprazole significantly prevented the development of reflux oesophagitis.

Cephradine (Anspor) is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.

OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.

OTS514 hydrochloride is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM).

OTS514 (OTS514 Hydrochloride) is a potent TOPK inhibitor. OTS514 exhibits a growth-suppressive effect on small cell lung cancer. OTS514 effectively suppressed the growth of SCLC cell lines (IC50: 0.4 ~ 42.6 nM). Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity. OTS514 treatment reduced CD90-positive SCLC cells and showed a higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.

Ilaprazole sodium (IY-81149 sodium) , a substituted benzimidazole prodrug, is a selective and irreversible proton pump inhibitor. A weak base, Ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+ K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

TOPK-p38 JNK-IN-1 (Compound B12) is an orally active inhibitor of the TOPK-p38 JNK signaling pathway, exhibiting an IC50 of 2.14 μM for NO production inhibition. It demonstrates anti-inflammatory properties by inhibiting downstream protein phosphorylation and preventing TOPK degradation [1].

OTS964 is a potent, orally active compound that operates as a highly selective inhibitor of TOPK with an IC 50 of 28 nM [1]. Additionally, it demonstrates significant inhibitory action against cyclin-dependent kinase CDK11, specifically binding to CDK11B with a K d of 40 nM [2].

ADA-07 is a TOPK inhibitor which interacts with TOPK at the ATP-binding pocket and inhibits its kinase activity, thereby suppressing SUV-induced phosphorylation of ERK1/2, p38, and JNKs, and subsequently inhibiting AP-1 activity.

Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor that irreversibly inhibits H+ K+-ATPase in rabbit parietal cells with a dose-dependent IC50 of 6 μM. It is used in gastric ulcer research and acts as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) [1] [2].