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SML1911

Sigma-Aldrich

INI-43

≥98% (HPLC)

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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
Empirical Formula (Hill Notation):
C22H23N7
CAS Number:
Molecular Weight:
385.46
NACRES:
NA.77

Quality Level

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

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This Item
SML0412SML1762B8810
INI-43 ≥98% (HPLC)

Sigma-Aldrich

SML1911

INI-43

IM-54 ≥98% (HPLC)

Sigma-Aldrich

SML0412

IM-54

SI-2 ≥98% (HPLC)

Sigma-Aldrich

SML1762

SI-2

BAY 41-2272 ≥97% (HPLC)

Sigma-Aldrich

B8810

BAY 41-2272

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

light orange to dark orange

color

, light yellow to dark orange

color

white to light brown

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 5 mg/mL (clear solution)

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

Quality Level

100

Quality Level

-

Quality Level

100

Quality Level

-

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

Signal Word

Warning

Hazard Statements

Hazard Classifications

Skin Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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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)
Targeting the nuclear import receptor, Kpn beta as an anti-cancer therapeutic
Watt VD, et al.
Molecular Cancer Therapeutics, molcanther-molcan0052 (2016)
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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