4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol
B022
CAS: 1202764-53-1
Molecular Formula: C19H16ClN5OS
4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol - Names and Identifiers
4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol - Physico-chemical Properties
| Molecular Formula | C19H16ClN5OS |
| Molar Mass | 397.88 |
| Appearance | Solid |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | 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. 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. |
| In vivo study | 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. |
4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol - Reference Information
| Biological activity | B022 is an effective selective NF-κB inducible kinase (NIK) inhibitor with Ki of 4.2 nM. B022 protects the liver from inflammation, oxidative stress and injury caused by toxins. |
| target | Ki: 4.2 nM (NF-κB-indexing kinase (NIK)) |
| in vitro study | B022 (0-5μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner. B022 (0-5μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5. Western Blot Analysis Cell Line: hepa1 cells Concentration: 0 μ m, 0.5 μ m, 5 μ m Incubation time: 12 hours result: Suppressed NIK-induced p52 formation in a dose-dependent banner. RT-PCR cell line: Hepa1 cells Concentration: 0 μ m, 0.5 μ m, 5 μ m 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. |
| Cell Line: | Hepa1 cells Hepa1 cells |
| Concentration: | 0 μM, 0.5 μM, 5 μM 0 μM, 0.5 μM, 5 μM |
| Incubation Time: | 12 hours 12 hours |
| Result: | Suppressed NIK-induced p52 formation in a dose-dependent manner. 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. 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. |
| in vivo study | B022 (30 mg/kg; intravenous injection; two 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; two 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. |
| 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 |
Last Update：2024-04-09 21:04:16
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CAS: 1202764-53-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
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Wechat: 15671228036
CAS: 1202764-53-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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