2. Immunology/Inflammation Apoptosis
  3. AP-1 Apoptosis
  4. INI-43

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.

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INI-43

INI-43 Chemical Structure

CAS No. : 881046-01-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

INI-43 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE INI-43

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c-Fos FosB Fra1/FOSL1 Fra2/FOSL2 c-Jun

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Description

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].

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

INI-43 Related Antibodies

Cell Proliferation Assay[3]

Cell Line: CaSki, HeLa, Kyse30, WHCO6, DMB and FG0 cells
Concentration: 5, 10 μmol/L
Incubation Time: 5 days
Result: At a concentration of 10 μmol/L, in less than 24 hours, the activity of cancer cells was significantly reduced, and within 48 to 72 hours, the cells were completely dead.

Western Blot Analysis[3]

Cell Line: HeLa cells
Concentration: 10, 15 μmol/L
Incubation Time: 1.5, 3h
Result: Prevented NFY from entering the nucleus.
Cytochrome C levels in mitochondria decreased, activating endogenous apoptotic pathways, and caspase-3/7 activity significantly increased.

Western Blot Analysis[2]

Cell Line: HeLa and SiHa cells
Concentration: 5 μM
Incubation Time: 2h
Result: Has a synergistic effect with Cisplatin, can inhibit Kpnβ1, increase the stability of p53, reduce the nuclear localization of NFκB and its target expression in SiHa cells after Cisplatin treatment, and enhance the DNA damage after Cisplatin treatment.

Immunofluorescence[3]

Cell Line: HeLa cells
Concentration: 10 μmol/L
Incubation Time: 1.5, 3h
Result: Prevented p65 from entering the nucleus.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

385.46

Formula

C22H23N7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=C(C2=NC3=CC=CC=C3N=C2N1CCCN(C)C)C4=NC5=CC=CC=C5N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (259.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5943 mL 12.9715 mL 25.9430 mL 64.8576 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 mL 12.9715 mL
10 mM 0.2594 mL 1.2972 mL 2.5943 mL 6.4858 mL
15 mM 0.1730 mL 0.8648 mL 1.7295 mL 4.3238 mL
20 mM 0.1297 mL 0.6486 mL 1.2972 mL 3.2429 mL
25 mM 0.1038 mL 0.5189 mL 1.0377 mL 2.5943 mL
30 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1619 mL
40 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6214 mL
50 mM 0.0519 mL 0.2594 mL 0.5189 mL 1.2972 mL
60 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0810 mL
80 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.8107 mL
100 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6486 mL
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INI-43 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INI-43881046-01-1INI43INI 43AP-1ApoptosisActivator Protein 1Kpnβ1 cargoesNFATNFκBNFY Cervical cancer Nuclear importcervical tumorxenografted esophagealInhibitorinhibitorinhibit

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