所有图片(1)
别名:
3-氨基-6-(4-(甲磺酰基)苯基)-N-苯基吡嗪-2-甲酰胺, 3-氨基-6-[4-(甲磺酰基)苯基]-N-苯基-2-吡嗪甲酰胺, VE821
经验公式（希尔记法）:
C18H16N4O3S
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: ≥10 mg/mL, clear
储存温度
−20°C
SMILES字符串
CS(C(C=C1)=CC=C1C2=NC(C(NC3=CC=CC=C3)=O)=C(N)N=C2)(=O)=O
InChI
1S/C18H16N4O3S/c1-26(24,25)14-9-7-12(8-10-14)15-11-20-17(19)16(22-15)18(23)21-13-5-3-2-4-6-13/h2-11H,1H3,(H2,19,20)(H,21,23)
InChI key
DUIHHZKTCSNTGM-UHFFFAOYSA-N
应用
VE-821 已用作人癌细胞中 ATM 和 Rad3 相关（ATR）蛋白的抑制剂。
生化/生理作用
VE-821 是一种有效的 ATP 竞争性抑制剂，可抑制 DNA 损伤应答（DDR）激酶共济失调毛细血管扩张突变（ATM）以及与 ATM 和 Rad3 相关（ATR），Ki 值为 13 nM。VE-821 对相关 PIKKs ATM、DNA 依赖性蛋白激酶（DNA-PK）、mTOR 和 PI3-激酶-γ 的交叉反应极小（Ki 值分别为 16 μM、2.2 μM、>1 μM 和 3.9 μM），并针对大量无关的蛋白激酶。在大部分癌细胞中单独使用 VE-821 会导致细胞死亡，并且还显示出与遗传毒性剂的强大协同作用。VE-821 增加了细胞对放射线的敏感性，并使癌细胞对多种化学治疗剂敏感。
其他说明
VE-821 已由化学探针门户网站进行了专家审查和推荐。有关更多信息，请访问化学探针门户网站上的 VE-821 探针摘要。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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