864420-54-2
中文名称
化合物NAE-IN-M22
英文名称
NEDD8 inhibitor M22
CAS
864420-54-2
分子式
C20H24Cl2N2
分子量
363.32
MOL 文件
864420-54-2.mol
更新日期
2024/07/23 09:41:46
864420-54-2 结构式
基本信息
中文别名
化合物NAE-IN-M22 英文别名
NAE-IN-M22NEDD8 inhibitor M22
4-Piperidinamine, N-[2-(2,4-dichlorophenyl)ethyl]-1-(phenylmethyl)-
NAEINM22,cancer,Inhibitor,NAE-IN-M-22,NAE,NEDD8,NAE IN M22,enzyme,activating,inhibit,tumor,Apoptosis
常见问题列表
生物活性
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。靶点
NEDD8 activating enzyme (NAE)
体外研究
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. |
体内研究
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.