1. 疾病领域
  2. 癌症
  3. SMDC818909

SMDC818909 是一种吲哚酰胺类、靶向 p97 AAA+ ATPase 的反竞争性抑制剂,IC50=3.5 μM,Ka=9.1 μM。SMDC818909 可结合 p97D2 ATPase 结构域,优先结合 p97ADP 结合构象,以别构方式阻断 p97 的 ATP 水解循环,抑制其介导的细胞内蛋白稳态调控功能。SMDC818909 应用于靶向p97的抗肿瘤药物研发,以及癌症相关的蛋白毒性应激机制研究。

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SMDC818909

SMDC818909 Chemical Structure

CAS No. : 1147823-21-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms[1][2][3].

体外研究
(In Vitro)

SMDC818909 与全长 p97 的 D2 结构域结合,Kd 为 9.1 μM[1]
SMDC818909 (5-100 μM ATP) 是 p97 ATP 酶的非竞争性抑制剂,在 5、20、100 μM ATP 条件下的 IC50 分别为 26 μM、11.5 μM、4.9 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

267.29

Formula

C14H13N5O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

SMDC818909 相关分类

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SMDC818909
目录号:
HY-124253
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