2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor PI3K/Akt/mTOR Apoptosis
  3. RAR/RXR PI3K Akt Apoptosis
  4. K-8012

K-8012 是一种 sulindac (HY-B0008) 类似物，是 RXRa 的有效拮抗剂。K-8012 抑制 9-cis-RA 诱导的 Gal4-RXRa-LBD 反式激活的 IC50 值约为 9.2 μM。K-8012 以 RXRa 依赖性方式发挥优于 sulindac 的抗癌活性。K-8012 表现出抑制 tRXRa 介导的 PI3K/AKT 信号通路的活性。K-8012 通过阻止 tRXRa 与 p85a 结合来诱导细胞凋亡并抑制 AKT 激活。

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K-8012 Chemical Structure

K-8012 Chemical Structure

CAS No. : 1346513-17-4

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规格 价格 是否有货 数量
1 mg ￥1785
1 - 2 周
5 mg ￥4130
1 - 2 周
10 mg 现货 1 - 2 周
50 mg   询价  
100 mg   询价  

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K-8012 相关抗体

Top Publications Citing Use of Products

查看 RAR/RXR 亚型特异性产品:

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RXRα RXRβ RXRγ

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a[1].

IC50 & Target

RXR α

 

分子量

374.45

Formula

C23H23FN4
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

K-8012 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

K-80121346513-17-4K8012K 8012RAR/RXRPI3KAktApoptosisRetinoic acid receptorsRetinoid X receptorsPhosphoinositide 3-kinasePKBProtein kinase Banti-cancerRetinoid X receptor-alphaInhibitorinhibitorinhibit

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目录号：
HY-121435
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