化合物NAE-IN-M22
| 中文名称 | 化合物NAE-IN-M22 |
|---|---|
| 中文同义词 | 化合物NAE-IN-M22;NEDD8抑制剂M22 |
| 英文名称 | NEDD8 inhibitor M22 |
| 英文同义词 | NEDD8 inhibitor M22;4-Piperidinamine, N-[2-(2,4-dichlorophenyl)ethyl]-1-(phenylmethyl)-;NAE-IN-M22;NAEINM22,cancer,Inhibitor,NAE-IN-M-22,NAE,NEDD8,NAE IN M22,enzyme,activating,inhibit,tumor,Apoptosis |
| CAS号 | 864420-54-2 |
| 分子式 | C20H24Cl2N2 |
| 分子量 | 363.32 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 864420-54-2.mol |
| 结构式 |  |
化合物NAE-IN-M22 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：250 mg/mL（688.10 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
NAE-IN-M22 是一种有效，选择性和可逆的 NEDD8 活化酶 (NAE) 抑制剂，效力在微摩尔范围内。NAE-IN-M22 抑制多种癌细胞生长并诱导 A549 细胞凋亡。NAE-IN-M22 还可以在体内抑制肿瘤的生长。
NEDD8 activating enzyme (NAE)
M22 (0.37-90 μM; 24 h) blocks neddylation pathway selectively and suppresses degradation of CRL substrates in A549 cells.
M22 (0.1-100 μM; 48 h) inhibits A549 cell proliferation completely at 30 µM (GI
50
=5.5 µM, GI
90
=19.3 µM).
M22 (15-30 μM; 36 h) promotes apoptosis in A549 cell line.
Cell Viability Assay
| Cell Line: | A549 cells |
| Concentration: | 0.37, 1.11, 3.33, 10, 30, 90 μM |
| Incubation Time: | 24 hours |
| Result: |
Inhibited formations of Uba3-NEDD8 and Ubc12-NEDD8.
Resulted in a corresponding decrease in the abundance of Cullins-NEDD8. Decreased the degradations of p27 and CDT1. Prevented p53 from degradation. |
M22 (60 mg/kg; i.p. once daily for 14 d) inhibits tumor growth in nude mice bearing AGS xenografts.
M22 (0.36-90 μM) has low acute toxicity in zebrafish model.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-115537 | NAE-IN-M22 | 1 mg | 960元 | |
| 2024/04/30 | HY-115537 | 化合物NAE-IN-M22 NAE-IN-M22 | 864420-54-2 | 5mg | 2400元 |