2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  3. IRE1 PDGFR c-Kit
  4. AK177

AK177 是一种 IRE1α 核糖核酸酶变构激活剂，对非磷酸化和磷酸化的 IRE1α 分别为 480 和 180 nM。

AK177 能够浓度依赖性地促进 IRE1α 切割 XBP1 mRNA 探针，并能稳定结合其激酶结构域。但 AK177​ 激酶选择性差，且在细胞水平上由于膜渗透性不佳，导致下游通路激活和抗增殖活性均不显著。

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AK177

AK177 Chemical Structure

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AK177 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

AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively.\n

AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity[1].
体外研究
(In Vitro)

AK177 可在无细胞 HTRF 实验中抑制 PDGFRA 激酶活性，其 IC50 为 9.0 nM[1]。
AK177 可在无细胞 HTRF 分析中以 113.7 nM 的 IC50 抑制 KIT 激酶活性[1]。
AK177 在无细胞激酶组分析实验中可抑制 85 种受试激酶中 49 种的活性[1]。
AK177 (0.25-20 μM; 24 h) 可在 MCF-7 细胞中微弱诱导 XBP1 mRNA 剪接，20 μM 处理 24 h 后激活倍数不足 2 倍[1]。
AK177 (0.25-20 μM; 24 h) 不会在 MCF-7 细胞中通过 RIDD 诱导可检测到的 Bloc1s1 mRNA 降解，处理浓度最高达 20 μM、处理时间为 24 h[1]。
AK177 (1-100 μM; 72 h) 在浓度高达 100 μM、处理 72 h 后，对 HT-29、MDA-MB-231 和 MCF-7 细胞的细胞活力无显著抑制作用[1]。

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

AK177 相关抗体:

Real Time qPCR[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0.25, 0.77, 2.22, 6.67 and 20 μM
Incubation Time: 24 h
Result: Induced less than 2-fold increase in XBP1s mRNA levels at the highest tested concentration of 20 μM, with minimal concentration-dependent changes across all tested doses.\nDid not cause significant changes in Bloc1s1 mRNA levels at any tested concentration.
分子量

564.62

Formula

C26H28N8O5S
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

AK177 相关分类

  • 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.

Keywords:

AK177AK 177AK-177IRE1PDGFRc-KitInositol requiring enzyme 1Platelet-derived growth factor receptorSCFRCD117IRE1α kinase domainPDGFRA kinaseKIT kinaseHT-29 cellsphosphorylated IRE1αMCF-7 cellsXBP1 mRNAMDA-MB-231 cellsIRE1α ribonucleaseunphosphorylated IRE1αInhibitorinhibitorinhibit

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产品名称：
AK177
目录号：
HY-181886
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