B022

Research use only, not for human use.

B022 is a selective and potent NF-κB-induced kinase (NIK) inhibitor (Ki: 4.2 nM) and a chemical probe for treating liver inflammation and injury, protecting the liver from inflammation and injury caused by oxidative stress and toxins.

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.

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.

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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Apoptosis

NF-κB

NF-κB

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1202764-53-1

397.88

C19H16ClN5OS

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (628.33 mM; Ultrasonic )

CC(O)(C#Cc1ccc2CCN(c2c1)c1nc(N)ncc1Cl)c1nccs1

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(-20℃)

With Ice Pack

≥ 2 years