1. Metabolic Enzyme/Protease
  2. 17β-HSD
  3. CRT0083914

CRT0083914 (compound 12) 是 AKR1C3 的亚型选择性非羧酸盐类抑制剂。CRT0083914 可用于结肠癌的研究。

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CRT0083914

CRT0083914 Chemical Structure

CAS No. : 932495-16-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CRT0083914 (compound 12) is a subtype-selective non-carboxylate inhibitor of AKR1C3. CRT0083914 is applicable to the research of colon cancer[1].

体外研究
(In Vitro)

CRT0083914 (0.1 nM to 100 μM) 可强效且选择性地抑制重组人源 AKR1C3 酶,其 IC50 为 0.094 μM;而在测试浓度下,该化合物对 AKR1C1、AKR1C2、AKR1C4、COX-1 或 COX-2 均无活性[1]
CRT0083914 可在过表达 AKR1C3 的 HCT-116 细胞中抑制 AKR1C3 依赖性 PR-104A 代谢,其 IC50 为 11 nM[1]
CRT0083914 以其 2-吡咯烷酮结合 AKR1C3 的 SP3 口袋,以其含磺酰胺的基团结合 SP1 口袋,与该酶的氧阴离子空穴残基无直接接触[1]

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

分子量

322.42

Formula

C16H22N2O3S

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
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产品名称:
CRT0083914
目录号:
HY-123732
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