| Identification | Back Directory | [Name]
3-(1H-benzimidazol-2-yl)-1-[3-(dimethylamino)propyl]pyrrolo[3,2-b]quinoxalin-2-amine | [CAS]
881046-01-1 | [Synonyms]
INI43
INI-43
INI 43
INI-43 >=98% (HPLC)
INI-43,NFκB,NFY,AP-1,Inhibitor,inhibit,NFAT,Kpnβ1 cargoes
3-(1H-benzimidazol-2-yl)-1-[3-(dimethylamino)propyl]pyrrolo[3,2-b]quinoxalin-2-amine
1H-Pyrrolo[2,3-b]quinoxaline-1-propanamine, 2-amino-3-(1H-benzimidazol-2-yl)-N,N-dimethyl- | [Molecular Formula]
C22H23N7 | [MDL Number]
MFCD06650809 | [MOL File]
881046-01-1.mol | [Molecular Weight]
385.46 |
| Chemical Properties | Back Directory | [Boiling point ]
684.4±65.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 10mg/mL, clear | [form ]
Solid | [pka]
10.80±0.10(Predicted) | [color ]
Light yellow to yellow | [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(N)=C(C2=NC3=C(C=CC=C3)N2)C(C1=N4)=NC5=C4C=CC=C5 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import th at cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as th at of its cargo transcription factorsNFYAP-1p65and 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 activityinduced by phorbol-12-myristate-13-acetate (PMA). | [in vivo]
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].
| Animal Model: | WHCO6 esophageal cancer or CaSki cervical cancer cells mouse xenografts models[3] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Significantly inhibited the growth of esophageal and neck tumors. |
| [References]
[1] F J Stanfield, et al. The antiviral activity of caprochlorone. Proc Soc Exp Biol Med. 1967 May;125(1):297-303. DOI:10.3181/00379727-125-32076
[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. DOI:10.1186/s12885-021-07819-3
[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. DOI:10.1158/1535-7163.MCT-15-0052 |
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