SML1911
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:
Molecular Weight:
385.46
UNSPSC Code:
12352200
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
InChI
1S/C22H23N7/c1-28(2)12-7-13-29-20(23)18(21-25-15-9-4-5-10-16(15)26-21)19-22(29)27-17-11-6-3-8-14(17)24-19/h3-6,8-11H,7,12-13,23H2,1-2H3,(H,25,26)
InChI key
LWPQQQAILAUWTI-UHFFFAOYSA-N
Biochem/physiol Actions
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).
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 a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import.
signalword
Warning
hcodes
Hazard Classifications
Skin Irrit. 2
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML1911-25MG | 04061833265550 |
| SML1911-5MG | 04061833265567 |