4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇
| 中文名称 | 4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇 |
|---|---|
| 中文同义词 | 4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇;B022;化合物 T14491 |
| 英文名称 | 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol |
| 英文同义词 | 4-(1-(2-amino-5-chloropyrimidin-4-yl)-2-(thiaol-2-yl)but-30-yn-2-ol;B022;2-Thiazolemethanol, α-[2-[1-(2-amino-5-chloro-4-pyrimidinyl)-2,3-dihydro-1H-indol-6-yl]ethynyl]-α-methyl-;B022,B-022 |
| CAS号 | 1202764-53-1 |
| 分子式 | C19H16ClN5OS |
| 分子量 | 397.88 |
| EINECS号 | |
| 相关类别 | 活性分子 |
| Mol文件 | 1202764-53-1.mol |
| 结构式 |  |
4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇 性质
| 沸点 | 644.4±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.53±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：250 mg/mL（628.33 mM） |
| 酸度系数(pKa) | 10.71±0.29(Predicted) |
B022 是一种有效的选择性的 NF-κB 诱导激酶 (NIK) 抑制剂，Ki 为 4.2 nM。B022 可保护肝脏免受毒素引起的炎症，氧化应激和伤害。
Ki: 4.2 nM (NF-κB-inducing kinase (NIK))
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-120501 | B022 | 1 mg | 931元 | |
| 2024/01/25 | HY-120501 | 4-(1-(2-氨基-5-氯嘧啶-4-基)-2-(噻唑-2-基)-3-丁炔-2-醇 B022 | 1202764-53-1 | 5mg | 2050元 |