IKK-16 (IKK Inhibitor VII) |
Katalog-Nr.GC12180
One-Click Copy Product Info
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IKK-16 (IKK-Inhibitor VII) ist ein selektiver IκB-Kinase (IKK)-Inhibitor fÜr IKK2, den IKK-Komplex und IKK1 mit IC50-Werten von 40 nM, 70 nM bzw. 200 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 873225-46-8
Sample solution is provided at 25 µL, 10mM.
IKK-16 (IKK Inhibitor VII) is a novel, orally active selective inhibitor of IκB kinase (IKK), with IC₅₀ values of 40nM, 70nM, and 200nM against IKK-2, IKK complex, and IKK-1[1-2]. IKK-16 shows potential applications in research areas such as sepsis, acute inflammation models, and prostate cancer[3-4].
In vitro, treatment of SKBR3 cells with 5µM IKK-16 for 24 hours significantly inhibited cell viability, reduced interactions between PTPIP51 and RelA/IκB, enhanced the association of PTPIP51 with the Her2 receptor, and weakened the interaction between PTPIP51 and PTP1B[5]. In HepG2 cells, combined treatment with 5µM IKK-16 and deoxyelephantopin (DET; 10–100µM) for 24 hours, IKK-16 further enhanced DET-induced cytotoxicity and synergistically suppressed nuclear translocation of NF-κB p65[6].
In vivo, in LPS/PepG-induced multiple organ dysfunction models and cecal ligation and puncture (CLP)-induced sepsis models, intravenous administration of IKK-16 (1mg/kg) 1 hour after induction, IKK-16 significantly alleviated sepsis-related cardiac dysfunction, renal impairment, hepatocellular injury, and pulmonary inflammation. IKK-16 also reduced phosphorylation of IκBα, nuclear translocation of NF-κB p65 subunit, and expression of inducible nitric oxide synthase (iNOS) in cardiac and hepatic tissues[7]. In a 5/6 nephrectomy-induced chronic kidney disease (CKD) mouse model, intravenous administration of IKK-16 (1mg/kg) 1 hour after LPS challenge (2mg/kg) or CLP surgery, IKK-16 markedly attenuated sepsis-aggravated cardiac dysfunction and pulmonary inflammation, lowered plasma levels of proinflammatory cytokines (TNF-α, IL-1β, IL-6, IL-10), and suppressed phosphorylation of IKKα/β and IκBα, nuclear translocation of p65 NF-κB, and iNOS expression in cardiac tissues[8].
References:
[1] Waelchli R, Bollbuck B, Bruns C, et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12.
[2] Mu Y, Cory TJ. Suppression of HIV-1 Viral Replication by Inhibiting Drug Efflux Transporters in Activated Macrophages. Curr HIV Res. 2021;19(2):128-137.
[3] Galbraith NJ, Manek S, Walker S, et al. The effect of IκK-16 on lipopolysaccharide-induced impaired monocytes. Immunobiology. 2018 Apr-May;223(4-5):365-373.
[4] Zhang K, Yang J, Yang QQ, et al. ER stress genes (COL1A1, LOXL2, VWF) predicts IKK-16 as a Candidate therapeutic target for colitis-related inflammation and fibrosis suppression. Front Immunol. 2025 Jun 18;16:1587860.
[5] Dietel E, Brobeil A, Tag C, et al. PTPIP51 crosslinks the NFκB signaling and the MAPK pathway in SKBR3 cells. Future Sci OA. 2020 Mar 4;6(5):FSO463.
[6] Mehmood T, Maryam A, Zhang H, et al. Deoxyelephantopin induces apoptosis in HepG2 cells via oxidative stress, NF-κB inhibition and mitochondrial dysfunction. Biofactors. 2017 Jan 2;43(1):63-72.
[7] Coldewey SM, Rogazzo M, Collino M, et al. Inhibition of IκB kinase reduces the multiple organ dysfunction caused by sepsis in the mouse. Dis Model Mech. 2013 Jul;6(4):1031-42.
[8] Chen J, Kieswich JE, Chiazza F, et al. IκB Kinase Inhibitor Attenuates Sepsis-Induced Cardiac Dysfunction in CKD. J Am Soc Nephrol. 2017 Jan;28(1):94-105.
| Cell experiment [1]: | |
Cell lines | HepG2 cells (human hepatocellular carcinoma cell line) |
Preparation Method | HepG2 cells were cultured in Dulbecco’s Modified Eagle’s Medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 100U/mL penicillin, and 100μg/mL streptomycin at 37°C under 5% CO₂. Cells were treated with IKK-16 at 5μM, either alone or in combination with Deoxyelephantopin (DET; 30–50μM) or gemcitabine (GEM; 40–50μM) for 24 hours. |
Reaction Conditions | 5μM; 24 hours. |
Applications | IKK-16 significantly enhanced the cytotoxicity of DET and gemcitabine in HepG2 cells by further suppressing constitutive and TNF-α-induced NF-κB nuclear translocation. IKK-16 alone reduced NF-κB p65 subunit localization to the nucleus and synergized with DET to inhibit phosphorylation of IκBα, leading to increased apoptosis via mitochondrial dysfunction (e.g., cytochrome c release, caspase-3 activation, and PARP cleavage). |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice with chronic kidney disease (CKD) induced by 5/6 nephrectomy. |
Preparation Method | CKD mice were subjected to LPS-induced endotoxemia (2mg/kg; i.p.) or cecal ligation and puncture (CLP)-induced polymicrobial sepsis. IKK-16 (1mg/kg) was administered intravenously 1 hour after LPS injection or CLP surgery. Cardiac function, inflammatory markers, and organ injury were assessed at 18–24 hours. |
Dosage form | 1mg/kg; i.v.; Single injection. |
Applications | IKK-16 attenuated sepsis-aggravated cardiac dysfunction (improved ejection fraction, fractional shortening, and fractional area change), reduced lung inflammation (decreased myeloperoxidase activity), and suppressed systemic proinflammatory cytokine levels (TNF-α, IL-1β, IL-6, IL-10). Mechanistically, IKK-16 inhibited cardiac IKKα/β phosphorylation, IκBα degradation, NF-κB p65 nuclear translocation, and inducible nitric oxide synthase (iNOS) expression, while modulating Akt and ERK1/2 signaling pathways. |
References: | |
| Cas No. | 873225-46-8 | SDF | |
| Chemical Name | [4-[[4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone | ||
| Canonical SMILES | C1CCN(C1)C2CCN(CC2)C(=O)C3=CC=C(C=C3)NC4=NC=CC(=N4)C5=CC6=CC=CC=C6S5 | ||
| Formula | C28H29N5OS | M.Wt | 483.63 |
| Löslichkeit | ≥ 23.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0677 mL | 10.3385 mL | 20.677 mL |
| 5 mM | 413.5 μL | 2.0677 mL | 4.1354 mL |
| 10 mM | 206.8 μL | 1.0338 mL | 2.0677 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)