| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
INI-43 targets Kpnβ1 (karyopherin beta-1), a key mediator of nuclear import. It interferes with the nuclear localization of Kpnβ1 and its cargo proteins, including NFAT, NFκB, AP-1, and NFY. By blocking the nuclear import of these critical transcription factors, INI-43 disrupts oncogenic signaling pathways that are essential for cancer cell survival and proliferation.
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| ln Vitro |
In vitro, INI-43 shows significant cytotoxic effects on various cervical and esophageal cancer cell lines. It inhibits cancer cell proliferation, causes G2-M cell cycle arrest, and induces intrinsic apoptosis. At a concentration of 10 μmol/L, it significantly reduces cancer cell activity in less than 24 hours and leads to complete cell death within 48 to 72 hours. The IC50 for HeLa cells is 9.3 μmol/L. Notably, it shows selective cytotoxicity, killing cancer cells while having no effect on non-cancerous cells.
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| ln Vivo |
In vivo, INI-43 has demonstrated antitumor efficacy in mouse xenograft models of cancer. By inhibiting nuclear import of key transcription factors, it disrupts oncogenic signaling pathways and suppresses tumor growth. Its ability to target the nuclear transport machinery makes it a promising candidate for cancer therapy.
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| Enzyme Assay |
Kpnβ1 binding is assessed using biochemical assays such as surface plasmon resonance or isothermal titration calorimetry. The interaction between INI-43 and recombinant Kpnβ1 protein is measured to determine the binding affinity.
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| Cell Assay |
Cancer cell lines (e.g., HeLa, SiHa, CaSki, Kyse30) are treated with INI-43. Cell viability is measured using MTT or CellTiter-Glo assays. Cell cycle distribution is analyzed by flow cytometry, and apoptosis is detected by Annexin V staining or caspase activity assays. The compound's ability to reduce NFκB nuclear accumulation and downregulate target genes like cyclin D1, c-Myc, and XiAP is also assessed.
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| Animal Protocol |
In vivo efficacy is evaluated in nude mice bearing human tumor xenografts. INI-43 is administered intraperitoneally or orally, and tumor volume is measured over time. Tumor growth inhibition and markers of apoptosis and cell cycle arrest are assessed.
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| ADME/Pharmacokinetics |
INI-43 is expected to have favorable drug-like properties, including cell permeability and oral bioavailability. Its pharmacokinetic profile is consistent with a small molecule inhibitor targeting intracellular proteins. It is soluble in DMSO at 10 mg/mL.
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| Toxicity/Toxicokinetics |
Potential toxicities may include effects on normal cells that rely on Kpnβ1-mediated nuclear import for survival and proliferation. However, its selective cytotoxicity towards cancer cells suggests a favorable therapeutic window. GI toxicity and myelosuppression are possible class effects.
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| References | |
| Additional Infomation |
INI-43 is a research compound used to study the role of nuclear import in cancer and to validate Kpnβ1 as a therapeutic target. It represents a novel class of anticancer agents targeting the nuclear transport machinery. Its unique mechanism of action makes it a valuable tool for understanding the biology of nuclear transport and for developing new cancer therapies.
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| Molecular Formula |
C22H23N7
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|---|---|
| Molecular Weight |
385.46
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| Exact Mass |
385.201
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| CAS # |
881046-01-1
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| PubChem CID |
4910351
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
557
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2C(=CC=CC=2)N=C2C(C3NC4=CC=CC=C4N=3)=C(N)N(CCCN(C)C)C=12
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| InChi Key |
LWPQQQAILAUWTI-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-(1H-benzimidazol-2-yl)-1-[3-(dimethylamino)propyl]pyrrolo[3,2-b]quinoxalin-2-amine
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| Synonyms |
INI-43; INI43; INI 43
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~25.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5943 mL | 12.9715 mL | 25.9430 mL | |
| 5 mM | 0.5189 mL | 2.5943 mL | 5.1886 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5943 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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