2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. IHMT-IDH1-053

IHMT-IDH1-053 (compound 16) 是一种高度选择性且不可逆的 IDH1 突变抑制剂，对 IDH1 R132H 的 IC50 为 4.7 nM。IHMT-IDH1-053 对 IDH1 wt 和 IDH2 wt/突变体表现出低活性。IHMT-IDH1-053 抑制 IDH1 R132H 突变体转染的 293T 细胞中 2-羟基戊二酸 (2-HG) 的产生 (IC50=28 nM)。IHMT-IDH1-053 通过与残基 Cys269 的共价键与 NAPDH 结合袋相邻的变构袋中的 IDH1 R132H 蛋白结合。IHMT-IDH1-053 抑制带有 IDH1 R132 突变体的 HT1080 细胞系和原代 AML 细胞的增殖。

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IHMT-IDH1-053 Chemical Structure

IHMT-IDH1-053 Chemical Structure

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IHMT-IDH1-053 相关抗体

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

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IDH1 IDH2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants[1].

IC50 & Target[1]

R132H IDH1

4.7 μM (IC50)

IDH1 wt

 

IDH2 wt

 

分子量

532.63

Formula

C25H33FN6O4S
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

IHMT-IDH1-053 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

Keywords:

IHMT-IDH1-053Isocitrate Dehydrogenase (IDH)IrreversibleIDH1-mutantIDH1 R132HIDH1 wtIDH2 wt2-HG293TNAPDHCys269HT1080 AMLInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-149359
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