For research use only. Not for therapeutic Use.
INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G2-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway[1][2][3].
INI-43 (5 μM, 2h) pretreatment n HeLa and SiHa cell lines of cervical cancer can effectively reduce the nuclear accumulation and activity of NFκB, resulting in decreased expression of cyclin D1, c-Myc and XIAP, and impaired DNA repair ability. Make cells more sensitive to Cisplatin[2].
INI-43 (10, 15 μmol/L, 1.5, 3h) interferes with the entry of Kpnβ1, NFAT, p65 and NFY into the nucleus and induces apoptosis in HeLa cells. The IC50 value of INI-43 against HeLa cells is 9.3 μmol/L[3].
INI-43 (5, 10 μmol/L, 5 days) has different sensitivity to cancer cell lines (cervical and esophageal cancer) and non-cancer lines (DMB and FG0), and INI-43 can kill cancer cells and has no effect on non-cancer cells[3].
INI-43 has good metabolic stability with a degradation half-life of more than 100 minutes and a maximum tolerable dose (MTD) of 50 mg/kg[3].
INI-43 (50 mg/kg, intrabitoneal injection, once every 2-3 days, for 3 to 4 weeks) can inhibit tumor growth in mouse tumor xenotransplantation model [3].
| Catalog Number | I029370 |
| CAS Number | 881046-01-1 |
| Synonyms | 3-(1H-benzimidazol-2-yl)-1-[3-(dimethylamino)propyl]pyrrolo[3,2-b]quinoxalin-2-amine |
| Molecular Formula | C22H23N7 |
| Purity | ≥95% |
| InChI | 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) |
| InChIKey | LWPQQQAILAUWTI-UHFFFAOYSA-N |
| SMILES | CN(C)CCCN1C(=C(C2=NC3=CC=CC=C3N=C21)C4=NC5=CC=CC=C5N4)N |
| Reference | [1]. F J Stanfield, et al. The antiviral activity of caprochlorone. Proc Soc Exp Biol Med. 1967 May;125(1):297-303. [2]. Chi RA, et al. Inhibition of Kpnβ1 mediated nuclear import enhances cisplatin chemosensitivity in cervical cancer. BMC Cancer. 2021 Feb 2;21(1):106. [3]. van der Watt PJ, et al. Targeting the Nuclear Import Receptor Kpnβ1 as an Anticancer Therapeutic. Mol Cancer Ther. 2016 Apr;15(4):560-73. |
