HI-TOPK-032, TOPK inhibitor

HI-TOPK-032 is a potent and selective TOPK inhibitor. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. 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. HI-TOPK-032 also inhibited anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. In vivo, administration of HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model. HI-TOPK-032 may be further developed as a potential therapeutic against colorectal cancer. The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell–originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation.

Product information

CAS Number: 487020-03-1

Molecular Weight: 369.40

Formula: C20H11N5OS

Chemical Name: N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide

Smiles: N#CC1C2=NC3=CC=CC=C3N=C2N2C=CC(=CC2=1)NC(=O)C1=CC=CS1

InChiKey: BCSBXWKRZUPFHW-UHFFFAOYSA-N

InChi: InChI=1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C) DMSO: 4 mg/mL(10.82 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Dong Joon Kim, et al. Cancer Res. 2012 Jun 15;72(12):3060-8.

Products are for research use only. Not for human use.