1. Cell Cycle/DNA Damage Cytoskeleton Membrane Transporter/Ion Channel
  2. PAK Potassium Channel
  3. PAK1-IN-3

PAK1-IN-3 是一种 PAK1 抑制剂,IC50 为 10 nM,对 PAK2IC50 为 20 nM,对 hERG 钾通道的 IC50 为 1079 nM。PAK1-IN-3 可通过定位正确的叔胺与 PAK1 中的 Asp106 形成盐桥。PAK1-IN-3 可抑制 PAK2hERG 钾通道。

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PAK1-IN-3

PAK1-IN-3 Chemical Structure

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Customer Review

查看 PAK 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

PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM, an IC50 of 20 nM against PAK2, and an IC50 of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels[1].

IC50 & Target[1]

PAK1

10 nM (IC50)

PAK2

20 nM (IC50)

体外研究
(In Vitro)

PAK1-IN-3 (Compound 12) 具有 3.02 的 logD7.4,在 PBS pH 7.4 中溶解度中等,血浆蛋白结合率高,在人肝细胞中具有类母体代谢稳定性,在 MDCKII 细胞中的外排率为 0.7,在 Caco-2 细胞中的外排率为 2.9[1]

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

分子量

535.04

Formula

C27H31ClN8O2

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
  • 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.

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产品名称:
PAK1-IN-3
目录号:
HY-182357
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