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 Chemical Structure

INI-43 Chemical Structure

CAS No. : 881046-01-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 175 In-stock
25 mg USD 350 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Based on 1 publication(s) in Google Scholar

INI-43 Related Antibodies

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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 : 10 mg/mL (25.94 mM; ultrasonic and warming and heat to 60°C; 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.

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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
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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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