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B022 Sale

(Synonyms: 4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇) 目录号 : GC39280

B022 是一种有效的选择性的 NF-κB 诱导激酶 (NIK) 抑制剂,Ki 为 4.2 nM。B022 可保护肝脏免受毒素引起的炎症,氧化应激和伤害。

B022 Chemical Structure

Cas No.:1202764-53-1

规格 价格 库存 购买数量
5mg
¥1,845.00
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10mg
¥3,150.00
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50mg
¥11,250.00
现货
100mg
¥19,800.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1].

[1]. Ren X, et al. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury. FASEB J. 2017 Feb;31(2):711-718.

Chemical Properties

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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1 mg 5 mg 10 mg
1 mM 2.5133 mL 12.5666 mL 25.1332 mL
5 mM 0.5027 mL 2.5133 mL 5.0266 mL
10 mM 0.2513 mL 1.2567 mL 2.5133 mL
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Research Update

Activation of NF-κB-Inducing Kinase in Islet β Cells Causes β Cell Failure and Diabetes

Mol Ther 2020 Nov 4;28(11):2430-2441.PMID:32730745DOI:10.1016/j.ymthe.2020.07.016.

Islet β cell death has been proved to contribute to diabetes. Studies suggest that the activation of nuclear factor κB (NF-κB)-inducing kinase (NIK) is involved in the β cell dysfunction encountered in obesity. However, the pathological significance of NIK activation in diabetes remains largely unknown. Here, we report that β cell-specific overexpression of NIK (β-NIK-OE) results in spontaneous diabetes in male mice at a young age (≥10 weeks of age), which is likely due to insulin deficiency, β cell death, and insulitis. Importantly, inhibiting the kinase activation of NIK by the small molecule B022 prevents NIK- or H2O2-induced β cell death and also reduces streptozotocin (STZ)-induced β cell death while ameliorating hyperglycemia, suggesting that the kinase activity of NIK is essential in inducing islet inflammation, β cell death, and diabetes. In all, this study not only uncovers a role of NIK in β cell failure but also provides a potential therapeutic target for the treatment of diabetes.

A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury

FASEB J 2017 Feb;31(2):711-718.PMID:27871061DOI:10.1096/fj.201600840R.

Potent and selective chemical probes are valuable tools for discovery of novel treatments for human diseases. NF-κB-inducing kinase (NIK) is a key trigger in the development of liver injury and fibrosis. Whether inhibition of NIK activity by chemical probes ameliorates liver inflammation and injury is largely unknown. In this study, a small-molecule inhibitor of NIK, B022, was found to be a potent and selective chemical probe for liver inflammation and injury. B022 inhibited the NIK signaling pathway, including NIK-induced p100-to-p52 processing and inflammatory gene expression, both in vitro and in vivo Furthermore, in vivo administration of B022 protected against not only NIK but also CCl4-induced liver inflammation and injury. Our data suggest that inhibition of NIK is a novel strategy for treatment of liver inflammation, oxidative stress, and injury.-Ren, X., Li, X., Jia, L., Chen, D., Hou, H., Rui, L., Zhao, Y., Chen, Z. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury.