1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. Mutant IDH1-IN-7

Mutant IDH1-IN-7 是一种高选择性 Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM,Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) 抑制剂。Mutant IDH1-IN-7 对野生型 IDH1、IDH2-wt 和 IDH2 R140Q 无抑制作用。Mutant IDH1-IN-7 抑制 U87-MG R132H 细胞中的 2-羟基戊二酸 (2-HG) 生成 (EC50 = 0.55 μM)。Mutant IDH1-IN-7 对 U87-MG R132H 和 HT-1080 细胞表现出中等程度的抗增殖作用。

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Mutant IDH1-IN-7

Mutant IDH1-IN-7 Chemical Structure

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查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells[1].

IC50 & Target[1]

R132H IDH1

0.26 μM (IC50)

R132H IDH1

2.1 μM (Kd)

R132C IDH1

1.1 μM (IC50)

体外研究
(In Vitro)

Mutant IDH1-IN-7 (Compound 13e) (10-40 μM, 72 小时) 对 U87-MG IDH1 R132H 和 HT-1080 细胞表现出中等程度的抗增殖活性,但在 U87-MG 和 L02 细胞中的效力明显降低[1]
Mutant IDH1-IN-7 (5 μM, 1 小时) 对野生型 IDH1、IDH2-wt 和 IDH2 R140Q 无抑制作用,IC50 值均> 40 μM[1]

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

分子量

456.54

Formula

C27H28N4O3

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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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Mutant IDH1-IN-7
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HY-175213
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