JHB-17
JHB-17 is an IKKβ inhibitor with blood-brain barrier permeability, with an IC50 of 1.1 μM and a KD of 1.293 μM. JHB-17 is a non-ATP competitive inhibitor targeting the allosteric site of IKKβ, and it inhibits the phosphorylation of IKKβ. JHB-17 promotes the nuclear translocation of Nrf2, upregulates the expression of HO-1, SLC7A11 and glutathione, and reduces ROS to exert antioxidant effects. JHB-17 reduces cerebral infarction volume and improves neurobehavioral function. JHB-17 can be used in the research of cerebral ischemia-reperfusion injury.
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- 分子式: C23H23Cl2NO3
- 分子量:432.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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IKKβ 1.1 μM (IC50) |
IKK-β 1.293 μM (Kd) |
HO-1 |
JHB-17 potently inhibits IKKβ kinase activity in a cell-free system with an IC50 of 1.1 μM, which is approximately 70 times more potent than EF24; it has a KD of 1.293 μM for binding to wild-type IKKβ, and its binding affinity to IKKβK428A and IKKβQ432A mutant proteins is reduced[1].
JHB-17 (0.625-5 μM; 1 h or 18 h) increases the survival rate of H2O2-damaged SH-SY5Y cells in a concentration-dependent manner[1].
JHB-17 (5 μM; 1 h or 18 h) significantly reduces lipid peroxidation levels (MDA levels) and ROS accumulation in SH-SY5Y cells damaged by H2O2 after 1 h or 18 h of pretreatment[1].
JHB-17 (5 μM; 6 h) promotes Nrf2 nuclear translocation[1].
JHB-17 (1.25-5 μM; 18 h) upregulates the expression of HO-1 protein in SH-SY5Y cells in a dose-dependent manner[1].
JHB-17 (5 μM; 18 h pretreatment, 6 h H2O2 exposure) inhibits H2O2-induced phosphorylation of IKKβ and upregulates the expression of HO-1 protein in SH-SY5Y cells after 18 h of pretreatment followed by 6 h of H2O2 exposure[1].
JHB-17 (5 μM; 18 h pretreatment, followed by 24 h H2O2 exposure) loses its cytoprotective effect against H2O2-induced damage in SH-SY5Y cells when IKKβ is overexpressed, which confirms that IKKβ is its key target[1].
JHB-17 acts in a dose-dependent manner, and this effect occurs after 18 h of pretreatment followed by 2 h of exposure to H2O2[1].
JHB-17 (1.25-5 μM; 18 h pretreatment, 24 h H2O2 exposure) upregulates the expression of SLC7A11, increases intracellular GSH levels and reduces lipid ROS, and inhibits H2O2-induced ferroptosis in SH-SY5Y cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y human neuroblastoma cells (H2O2-induced oxidative damage model)
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Concentration:0.625, 1.25, 2.5, 5 μM
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Incubation Time:1 h or 18 h (pretreatment); 24 h (H2O2 exposure)
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Result:Protected SH-SY5Y cells from H2O2-induced damage in a concentration-dependent manner for both 1 h and 18 h pretreatments, with significant protective activity observed at concentrations as low as 0.625 μM.
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Cell Line:SH-SY5Y cells
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Concentration:5 μM
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Incubation Time:6 h
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Result:Significantly enhanced Nrf2 fluorescence signal within the nuclei of SH-SY5Y cells, indicating increased Nrf2 nuclear translocation.
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Cell Line:SH-SY5Y cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:18 h
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Result:Dose-dependently increased HO-1 protein levels in SH-SY5Y cells after 18 h incubation.
At 5 μM, induced stronger HO-1 expression than JHA-7 and TBHQ.
Upregulated the expression of SLC7A11.
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Cell Line:SH-SY5Y cells (H2O2-induced oxidative damage model)
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Concentration:5 μM
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Incubation Time:18 h (pretreatment); 6 h (H2O2 exposure)
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Result:Significantly inhibited H2O2-induced IKKβ phosphorylation and upregulated HO-1 protein expression in SH-SY5Y cells.
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Cell Line:IKKβ-overexpressing SH-SY5Y cells exposed to H2O2
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Concentration:5 μM; 1200 ng/mL IKKβ plasmid
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Incubation Time:18 h (pretreatment); 24 h (H2O2 exposure); 6 h (transfection)
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Result:Significantly increased cell viability after H2O2 damage in cells with normal IKKβ expression.
Almost completely abolished this protective effect in IKKβ-overexpressing cells.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 15 mg/kg | i.p. | 7.57 h | 0.25 h | 56.3 ng/mL | 192.0 ng·h/mL | 205.0 ng·h/mL | 4.99 h | 7.19 h | 22.1 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 432.34
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分子式 C23H23Cl2NO3
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SMILES
O=C1/C(CC/C1=C\C2=CC=C(O)C(O)=C2)=C/C3=CC=C(N(CCCl)CCCl)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
JHB-17 関連分類
HY-184115 関連分類
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