Skip to Content
Merck
All Photos(1)

Key Documents

SML0796

Sigma-Aldrich

HI-TOPK-032

≥98% (HPLC)

Synonym(s):

N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C20H11N5OS
CAS Number:
487020-03-1
Molecular Weight:
369.40
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

orange to dark red

solubility

DMSO: 3 mg/mL, clear (warmed)

storage temp.

2-8°C

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)

InChI key

BCSBXWKRZUPFHW-UHFFFAOYSA-N

Application

HI-TOPK-032 has been used as a PDZ binding-kinase (PBK) inhibitor.

Biochem/physiol Actions

HI-TOPK-032 belongs to the class of ATP-competitive inhibitors. It can also be used as a potent therapeutic for colorectal cancer.
HI-TOPK-032 is a specific TOPK (T-LAK cell–originated protein kinase) inhibitor both in vitro and in vivo. HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

PBK/TOPK enhances aggressive phenotype in prostate cancer via β-catenin-TCF/LEF-mediated matrix metalloproteinases production and invasion.
Brown-Clay J D, et al.
Oncotarget, 6(17), 15594?15609-15594?15609 (2015)
Dong Joon Kim et al.
Cancer research, 72(12), 3060-3068 (2012-04-24)
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. Despite the identification of TOPK as a promising novel therapeutic target, no inhibitor of TOPK has
PBK/TOPK mediates geranylgeranylation signaling for breast cancer cell proliferation.
Dou X, et al.
Cancer Cell International, 15(1), 27-27 (2015)
Xiong Zhang et al.
Cancers, 13(7) (2021-05-01)
Metastatic castration-resistant prostate cancer (mCRPC) is a highly aggressive disease with few therapeutic options. Hyperactive androgen receptor (AR) signaling plays a key role in CRPC progression. Previously, we identified RAR-related orphan receptor gamma (RORγ) as a novel key driver of
Xiaoyan Dou et al.
Cancer cell international, 15, 27-27 (2015-03-10)
PDZ binding-kinase (PBK) (also named T-lymphokine-activated killer cell-originated protein kinase (TOPK)), a serine/threonine kinase, is tightly controlled in normal tissues but elevated in many tumors, and functions in tumorigenesis and metastasis. However, the signaling that regulates expression of PBK in

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service