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Sigma-Aldrich

INI-43

≥98% (HPLC)

Synonym(s):

2-Amino-3-(1H-benzimidazol-2-yl)-N,N-dimethyl-1H-pyrrolo[2,3-b]quinoxaline-1-propanamine, 3-(1H-Benzimidazol-2-yl)-1-(3-dimethylaminopropyl)pyrrolo[5,4-b]quinoxalin-2-amine, Inhibitor of Nuclear Import-43

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About This Item

Empirical Formula (Hill Notation):
C22H23N7
CAS Number:
881046-01-1
Molecular Weight:
385.46
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

CN(C)CCCN1C(N)=C(C2=NC3=C(C=CC=C3)N2)C(C1=N4)=NC5=C4C=CC=C5

Biochem/physiol Actions

INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT. INI-43 exhibit specific cytotoxicity toward cancer cells. INI-43 inhibits tumor growth in cancer xenograft models.
INI-43 is also known as (3-(1H-benzimidazol-2-yl)-1-(3-dimethylaminopropyl)pyrrolo[5,4-b]quinoxalin-2-amine). It has the ability to prevent the development of dermatologically xenografted esophageal and cervical tumor cells. INI-43 can also decrease activator protein 1 (AP-1) transcriptional activity, induced by phorbol-12-myristate-13-acetate (PMA).

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315

Hazard Classifications

Skin Irrit. 2

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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Targeting the nuclear import receptor, Kpn beta as an anti-cancer therapeutic
Watt VD, et al.
Molecular Cancer Therapeutics, molcanther-molcan0052 (2016)
KPNB1-mediated nuclear import is required for motility and inflammatory transcription factor activity in cervical cancer cells
Stelma T, et al.
Oncotarget, 8(20), 32833-32833 (2017)
Pauline J van der Watt et al.
Molecular cancer therapeutics, 15(4), 560-573 (2016-02-03)
Karyopherin beta 1 (Kpnβ1) is a nuclear transport receptor that imports cargoes into the nucleus. Recently, elevated Kpnβ1 expression was found in certain cancers and Kpnβ1 silencing with siRNA was shown to induce cancer cell death. This study aimed to

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