B022是一种强效且选择性的NF-κB-inducing kinase (NIK)抑制剂，IC50值为15.1nM。
Cas No.:1202764-53-1
Sample solution is provided at 25 µL, 10mM.
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B022 is a potent and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 value of 15.1nM [1]. B022 can prevent fat formation and inhibit the non-classical NF-κB signaling pathway, and reduce the phosphorylation level of RelA in the cytoplasm[2]. B022 has been widely used to inhibit the production of nitric oxide and alleviate liver damage[3].
In vitro, B022 treatment (20μM) for 48 hours significantly inhibited LTα1/β2-stimulated nuclear translocation of RelB and p52 in SNU-1196 cells[4]. Treatment with 10μM B022 for 16 hours significantly inhibited H2O2-induced cell death in INS-1 832/13 cells, and reversed the inhibitory effect of NIK on insulin secretion-related genes (such as Insulin1/2, Pdx-1, and Neurod1)[5].
In vivo, B022 was injected into the tail vein every 3 hours at the 25μg/kg dose for a total of 9 hours, which could alleviate the acute liver inflammation and damage induced by CCl4 in mice[6]. Intraperitoneal injection of 30mg/kg dose of B022 once a day for 10 consecutive days can alleviate the clinical symptoms of experimental autoimmune myasthenia gravis (EAMG) rats, reduce serum antibody levels, and improve the morphological changes at the neuromuscular junction and complement deposition[7].
References:
[1] Li Z, Li X, Su M B, et al. Discovery of a potent and selective NF-κB-inducing kinase (NIK) inhibitor that has anti-inflammatory effects in vitro and in vivo[J]. Journal of medicinal chemistry, 2020, 63(8): 4388-4407.
[2] Haselager M V, Eldering E. The therapeutic potential of targeting NIK in B cell malignancies[J]. Frontiers in immunology, 2022, 13: 930986.
[3] Zhang N, Shen S, Yang M, et al. Design, synthesis, and biological evaluation of a novel NIK inhibitor with anti-inflammatory and hepatoprotective effects for sepsis treatment[J]. Journal of Medicinal Chemistry, 2024, 67(7): 5617-5641.
[4] Xu K, Kessler A, Nichetti F, et al. Lymphotoxin beta‐activated LTBR/NIK/RELB axis drives proliferation in cholangiocarcinoma[J]. Liver international, 2024, 44(11): 2950-2963.
[5] Li X, Wu Y, Song Y, et al. Activation of NF-κB-inducing kinase in islet β cells causes β cell failure and diabetes[J]. Molecular Therapy, 2020, 28(11): 2430-2441.
[6] Ren X, Li X, Jia L, et al. A small‐molecule inhibitor of NF‐κB‐inducing kinase (NIK) protects liver from toxin‐induced inflammation, oxidative stress, and injury[J]. The FASEB Journal, 2017, 31(2): 711-718.
[7] Huang X, Zhang Z, Wang Z, et al. Targeting NF-kappaB-inducing kinase shapes B-cell homeostasis in myasthenia gravis[J]. Journal of Neuroinflammation, 2025, 22(1): 17.
B022是一种强效且选择性的NF-κB-inducing kinase (NIK)抑制剂，IC50值为15.1nM[1]。B022能阻止脂肪形成，抑制非经典NF-κB信号通路，并降低细胞质中RelA的磷酸化水平[2]。B022已被广泛用于抑制一氧化氮的产生和减轻肝脏损伤[3]。
在体外，使用20μM的B022处理SNU-1196细胞48小时，显著抑制了LTα1/β2刺激的RelB和p52的核转位[4]。使用1μM的B022处理INS-1 832/13细胞16小时，显著抑制了H2O2诱导的细胞死亡，并逆转了NIK对胰岛素分泌相关基因的抑制作用[5]。
在体内，以25μg/千克的剂量每3小时通过尾静脉注射B022一次，总计9小时，可减轻CCl4诱导的小鼠急性肝脏炎症和损伤[6]。每日一次腹腔注射30mg/kg剂量的B022，连续10天，可减轻实验性自身免疫性重症肌无力(EAMG)大鼠的临床症状，降低血清抗体水平，并改善神经肌肉接头处的形态学变化和补体沉积[7]。
| Cell experiment [1]: | |
Cell lines | INS-1 832/13 cells |
Preparation Method | INS-1 832/13 cells were cultured at 37°C and 5% CO2 in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and 50mM β-mercaptoethanol. INS-1 832/13 cells were treated with H2O2 (50μM) in the presence of B022 at different doses (0, 1, 5, and 10μM) for 16h and cell viability was measured. |
Reaction Conditions | 0, 1, 5, and 10μM; 16h |
Applications | B022 treatment significantly inhibited H2O2-induced cell death in INS-1 832/13 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Lewis rats |
Preparation Method | Female Lewis rats (6-8 weeks old) weighing 160-180g were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility with food and tap water ad libitum. The rats were provided with standard rat chow and water. The EAMG rat model was induced with rat AChR97-116 peptide (DGDFAIVKFTKVLLDYTGHI). The rats were immunized subcutaneously at the tail base with a total 200μl emulsion containing 75μg of rat AChR97-116 peptide in phosphate buffer saline emulsified in an equal volume of complete Freund’s adjuvant containing 1mg mycobacterium tuberculosis strain H37RA. Then, the rats were boosted on day 30 with the same dose of AChR97-116 peptide in incomplete Freund’s adjuvant. After the second immunization, clinical scores were assessed every day, and then we selected ongoing EAMG rats with onset clinical scores of 1-1.5 for therapeutic experiments. EAMG rats in the B022 group were intraperitoneally given 30mg/kg B022 for 10 days and the EAMG model group was injected with an equal volume of cosolvent. |
Dosage form | 30mg/kg/day for 10 days; i.p. |
Applications | B022 treatment alleviated the clinical symptoms of EAMG rats and exhibited protective consequences in the EAMG rat model. |
References: | |
| Cas No. | 1202764-53-1 | SDF | |
| 别名 | 4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇 | ||
| Canonical SMILES | CC(C1=NC=CS1)(C#CC2=CC3=C(CCN3C4=NC(N)=NC=C4Cl)C=C2)O | ||
| 分子式 | C19H16ClN5OS | 分子量 | 397.88 |
| 溶解度 | DMSO: 250 mg/mL (628.33 mM) | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5133 mL | 12.5666 mL | 25.1332 mL |
| 5 mM | 502.7 μL | 2.5133 mL | 5.0266 mL |
| 10 mM | 251.3 μL | 1.2567 mL | 2.5133 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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