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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CN(C)CCCN1C(N)=C(C2=NC3=C(C=CC=C3)N2)C(C1=N4)=NC5=C4C=CC=C5
生化／生理作用
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).
訊號詞
Warning
危險聲明
危險分類
Skin Irrit. 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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