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| 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol Basic information |
| 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol Chemical Properties |
Boiling point | 644.4±65.0 °C(Predicted) | density | 1.53±0.1 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO: 250 mg/mL (628.33 mM) | form | Solid | pka | 10.71±0.29(Predicted) | color | Light yellow to yellow |
| 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol Usage And Synthesis |
Biological Activity | B022 is a potent and selective NF-κB-inducible kinase (NIK) inhibitor with Ki of 4.2 nM. B022 protects the liver from inflammation, oxidative stress and damage caused by toxins. | 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. 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. | td> | 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. | tr> < /span> | 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. < /p> < tr> 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. | | target | Ki: 4.2 nM (NF-κB-inducing kinase (NIK)) |
| 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol Preparation Products And Raw materials |
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