1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide
| 中文名称 | 1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide |
|---|---|
| 中文同义词 | 化合物NRF2-IN-1;1-(4-(叔丁基)苄基)-3-(4-氯苯基)-N-羟基-1H-吡唑-5-甲酰胺;化合物NRF2-IN-1,10 MM DMSO 溶液 |
| 英文名称 | 1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide |
| 英文同义词 | 1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide;1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl);3-(4-Chlorophenyl)-1-[[4-(1,1-dimethylethyl)phenyl]methyl]-N-hydroxy-1H-pyrazole-5-carboxamide;Nrf2 inhibitor 1;1H-Pyrazole-5-carboxamide, 3-(4-chlorophenyl)-1-[[4-(1,1-dimethylethyl)phenyl]methyl]-N-hydroxy-;inhibit,Acute,leukemia,AML,myeloid,Nrf2,Inhibitor,Nrf2IN1,Keap1-Nrf2,Nrf-2-IN-1,Nrf2 IN 1;Nrf2-IN-1, 10 mM in DMSO |
| CAS号 | 1610022-76-8 |
| 分子式 | C21H22ClN3O2 |
| 分子量 | 383.87 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1610022-76-8.mol |
| 结构式 |  |
1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide 性质
| 密度 | 1.23±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：260 mg/mL（677.31 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.44±0.50(Predicted) |
| 颜色 | 白色至米白色 |
Nrf2-IN-1 是 Nrf2 的抑制剂，被用于急性髓性白血病 (AML) 药物研究。
Nrf2
Nrf2-IN-1 (Compound 4f) (10 μM) inhibits Nrf2 activation.
Nrf2-IN-1(1-20 μM; 48 hours) inhibits growth of the three AML cell.
Nrf2-IN-1 (5-10 μM; 48 hours) induces apoptosis of three AML cells in vitro.
Nrf2-IN-1 induces apoptotic signaling involving Bcl-2 and Bax.
Cell Viability Assay
| Cell Line: | THP-1 cells, HL-60 cells, U937 cells |
| Concentration: | 1 μM, 5 μM, 10 μM, 20 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited growth of the three AML cell types at 5 μM, 10 μM or 20 μM for 48 hours. |
Apoptosis Analysis
| Cell Line: | THP-1 cells, HL-60 cells, U937 cells |
| Concentration: | 5 μM, 10 μM |
| Incubation Time: | 48 hours |
| Result: | Induced apoptosis in AML cells in vitro. |
Western Blot Analysis
| Cell Line: | THP-1 cells, HL-60 cells, U937 cells |
| Concentration: | 5 μM, 10 μM |
| Incubation Time: | 48 hours |
| Result: | Triggered caspase-dependent apoptotic signaling in AML cells. |
Nrf2-IN-1 inhibits tumor growth via apoptosis in chicken eggs.