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Key Documents

SML0796

Sigma-Aldrich

HI-TOPK-032

≥98% (HPLC)

Synonym(s):

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

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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’.

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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
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
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

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