2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl
  4. GNF-6

GNF-6 (Compound 14) 抑制 BCR-ABL-T315I 的门控苏氨酸残基突变，对于 c-ABL-T334I、BCR-ABL 和 BCR-ABL-T315I 变体的 IC50 值分别为 0.25 μM、0.09 μM 和 0.590 μM。GNF-6 是一种 ATP 竞争性抑制剂，可破坏疏水性脊柱 (疏水性相互作用网络) 的组装，从而将激酶锁定在非活性“DFG-out”构象中。

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GNF-6 Chemical Structure

GNF-6 Chemical Structure

CAS No. : 839708-29-1

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GNF-6 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation[1].

分子量

456.42

Formula

C22H19F3N6O2
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

GNF-6 相关分类

  • 摩尔计算器

  • 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.

Keywords:

GNF-6839708-29-1GNF6GNF 6Bcr-Ablthreonine residueBCR-ABL-T315Ic-ABL-T334IBCR-ABLATP competitivehydrophobic spineDFG-outInhibitorinhibitorinhibit

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