1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. BRD2879

BRD2879 是一种有效的 IDH1-R132H 抑制剂,对 IDH1-R132H、IDH1-R132C、IDH1-WT 和 IDH2-R140Q 的 IC50 值分别为 0.05、2.5、>20、>20 µM。BRD2879 可降低 (R)-2-羟基戊二酸 (R-2HG) 水平。

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BRD2879 Chemical Structure

BRD2879 Chemical Structure

CAS No. : 1304750-47-7

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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

BRD2879 is a potent IDH1-R132H inhibitor with IC50 values of 0.05, 2.5, >20, >20 µM for IDH1-R132H, IDH1-R132C, IDH1-WT, IDH2-R140Q, respectively. BRD2879 reduces (R)-2-hydroxyglutarate (R-2HG) levels[1].

IC50 & Target[1]

R132H IDH1

0.05 μM (IC50)

R132C IDH1

2.5 μM (IC50)

IDH1 wt

>20 μM (IC50)

IDH2-R140Q

>20 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
> 20 μM
Compound: BRD2879
Inhibition of human C-terminal FLAG-tagged IDH1-R140Q mutant (1 to 452 residues) expressed in baculovirus infeceted sf9 cells assessed as inhibition of ketoreductase activity preincubated for 10 mins followed by addition of NADPH and alpha-KG as substrate
Inhibition of human C-terminal FLAG-tagged IDH1-R140Q mutant (1 to 452 residues) expressed in baculovirus infeceted sf9 cells assessed as inhibition of ketoreductase activity preincubated for 10 mins followed by addition of NADPH and alpha-KG as substrate
[PMID: 27774134]
分子量

571.70

Formula

C30H38FN3O5S

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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  • 稀释计算器

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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.

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产品名称:
BRD2879
目录号:
HY-120765
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