864420-54-2
中文名稱
化合物NAE-IN-M22
英文名稱
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
2024/12/22 16:36:04
864420-54-2 結(jié)構(gòu)式
基本信息
中文別名
化合物NAE-IN-M22 英文別名
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
常見問題列表
生物活性
NAE-IN-M22 是一種有效，選擇性和可逆的 NEDD8 活化酶 (NAE) 抑制劑，效力在微摩爾范圍內(nèi)。NAE-IN-M22 抑制多種癌細(xì)胞生長并誘導(dǎo) A549 細(xì)胞凋亡。NAE-IN-M22 還可以在體內(nèi)抑制腫瘤的生長。靶點
NEDD8 activating enzyme (NAE)
體外研究
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. |
體內(nèi)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.