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 |
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中文同义词 | 化合物NRF2-IN-1 |
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 |
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) |
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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
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.