1610022-76-8
中文名稱(chēng)
1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide
英文名稱(chēng)
1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide
CAS
1610022-76-8
分子式
C21H22ClN3O2
分子量
383.87
MOL 文件
1610022-76-8.mol
更新日期
2023/03/17 20:03:06
1610022-76-8 結(jié)構(gòu)式
基本信息
中文別名
化合物NRF2-IN-1 英文別名
Nrf2 inhibitor 11-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)
1-(4-(tert-butyl)benzyl)-3-(4-chlorophenyl)-N-hydroxy-1H-pyrazole-5-carboxamide
3-(4-Chlorophenyl)-1-[[4-(1,1-dimethylethyl)phenyl]methyl]-N-hydroxy-1H-pyrazole-5-carboxamide
1H-Pyrazole-5-carboxamide, 3-(4-chlorophenyl)-1-[[4-(1,1-dimethylethyl)phenyl]methyl]-N-hydroxy-
物理化學(xué)性質(zhì)
密度1.23±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 260 mg/mL (677.31 mM)
酸度系數(shù)(pKa)8.44±0.50(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
Nrf2-IN-1 是 Nrf2 的抑制劑，被用于急性髓性白血病 (AML) 藥物研究。靶點(diǎn)
Nrf2
體外研究
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. |
體內(nèi)研究
Nrf2-IN-1 inhibits tumor growth via apoptosis in chicken eggs.