For research use only. Not for therapeutic Use.
B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1][2]. B022 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1].?
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1].?
B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia[3].
B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses[1].
| Catalog Number | I017424 |
| CAS Number | 1202764-53-1 |
| Synonyms | 4-[1-(2-amino-5-chloropyrimidin-4-yl)-2,3-dihydroindol-6-yl]-2-(1,3-thiazol-2-yl)but-3-yn-2-ol |
| Molecular Formula | C19H16ClN5OS |
| Purity | ≥95% |
| InChI | InChI=1S/C19H16ClN5OS/c1-19(26,17-22-7-9-27-17)6-4-12-2-3-13-5-8-25(15(13)10-12)16-14(20)11-23-18(21)24-16/h2-3,7,9-11,26H,5,8H2,1H3,(H2,21,23,24) |
| InChIKey | OKFYOOFXVBCIIP-UHFFFAOYSA-N |
| SMILES | CC(C#CC1=CC2=C(CCN2C3=NC(=NC=C3Cl)N)C=C1)(C4=NC=CS4)O |
| Reference | [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. [2]. Li Z, 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 Med Chem. 2020;63(8):4388-4407. [3]. Li X, et al. Activation of NF-κB-Inducing Kinase in Islet β Cells Causes β Cell Failure and Diabetes. Mol Ther. 2020;28(11):2430-2441. |
