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You are here:Home-Inhibitors & Agonists-Ras-Raf-MAPK-ERK Pathway-TOPK

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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.

Cat. No. Product Name CAS No. Information
H7553

HI-TOPK-032

 		487020-03-1

A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity; also weakly inhibits MEK1 (40% inhibition at 5 uM); inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation; suppresses tumor growth in a colon cancer xenograft model.
H7552

ADA-07

 		2252153-94-7

A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis; interacts with TOPK at the ATP-binding pocket and inhibits its kinase activity; suppresses SUV-induced phosphorylation of ERK1/2, p38, and JNKs, and subsequently inhibits AP-1 activity; dramatically attenuates tumor incidence, multiplicity, and volume in SKH-1 hairless mice.
H7369

OTS-964 hydrochloride

 		1338545-07-5

OTS-964 is a dimethylated derivative of OTS514 and potent, selective TOPK inhibitor with IC50 of 28 nM, exhibits excellent in vivo efficacy with liposomal formulation; inhibits the growth of TOPK-positive cells with low IC50 values (A549 IC50=31 nM), decreases autophosphorylation of TOPK (Thr9), as well as phosphorylation of histone H3 (Ser10), in both T47D and LU-99 cells; the liposomal OTS964 causes complete regression of tumors without any detectable toxicity in the xenograft models.
H7555

SKLB-C05

SKLB-C05 is a novel selective, orally active TOPK inhibitor with IC50 of 0.5 nM, shows excellent cytotoxicity and anti-migration and invasion activity on TOPK high-expressing CRC cells and induces cell apoptosis; exhibits markedly prioritized inhibitory activity on TOPK-positive CRC cells than TOPK-negative cells (HCT116 cell IC50=96 nM); inhibits TOPK downstream signaling including ERK1/2, p38, and JNK1/2/3, as well as downregulation of FAK/Src- MMP signaling; dramatically attenuates CRC tumor xenograft growth and completely suppressed hepatic metastasis of HCT116 cells (20 and 10 mg/kg/day).
H7554

OTS-514

 		1338540-63-8

A highly potent and selective TOPK inhibitor with IC50 of 2.6 nM; shows selectivity against a panel of 60 kinases (at 0.2 uM, 11.5-18.5% inhibition); strongly suppresses the growth of TOPK-positive cancer cells; demonstrates in vivo efficacy but causes severe hematopoietic toxicity.

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