B022

SKU: orb2901622

Description

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. 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.

Key Properties

• CAS Number: 1202764-53-1
• MW: 397.88
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆ClN₅OS
• SMILES: CC(O)(C#Cc1ccc2CCN(c2c1)c1nc(N)ncc1Cl)c1nccs1
• Target: NF-κB
• Solubility: In Vitro: DMSO : 250 mg/mL (628.33 mM; Ultrasonic )

Bioactivity

• In Vivo:
  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. Animal model: STOP-NIK male mice (8 weeks) infected with Ad-cre. Dosage: 30 mg/kg. Administration: Intravenous injection; twice a day; for 10 days. Result: Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.
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• In Vitro:
  B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner. 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.B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia. Western blot analysis. Cell line: Hepa1 cells. Concentration: 0 μM, 0.5 μM, 5 μM Incubation time: 12 hours. Result: Suppressed NIK-induced p52 formation in a dose-dependent manner. RT-PCR Cell line: Hepa1 cells. Concentration: 0 μM, 0.5 μM, 5 μM Incubation time: 12 hours. Result: Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

NF-κB