1. Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage Cytoskeleton
  2. Interleukin Related TNF Receptor PAK
  3. PQA-18

PQA-18 是一种独特的 PAK2 抑制剂 (IC50: 10 nM)。PQA-18 具有免疫抑制活性,可抑制 IL2IL4IL6TNFα 产生。PQA-18 可抑制小鼠中调节性 T 细胞亚群的数量和针对 T 细胞依赖性抗原的免疫球蛋白 (Ig) 的产生,并可减轻小鼠的皮炎症状。

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PQA-18 Chemical Structure

PQA-18 Chemical Structure

CAS No. : 1604678-82-1

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规格 价格 是否有货 数量
5 mg ¥1980
2 - 4 周
10 mg ¥2970
2 - 4 周
25 mg ¥5040
2 - 4 周
50 mg   询价  
100 mg   询价  

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice[1].

IC50 & Target[1]

PAK2

10 nM (IC50)

IL-6

 

IL4

 

IL-2

 

体外研究
(In Vitro)

PQA-18 (0.1-20 μM, 6-24 h) 抑制 ConA (HY-P2149) 诱导的人外周淋巴细胞中 IL2、IL4、IL6、TNFα 的产生 (IC50 分别为 450、650、580 和 460 nM) 和 Jurkat 细胞中 IL2 蛋白和 mRNA 产生 (IC50: 400 nM)[1]
PQA-18 (10 μM) 通过抑制相应的激酶来减弱 cofilin-1 和 histone H4 的磷酸化[1]
PQA-18 通过在 Ser141 处的自磷酸化抑制 PAK2 的活性[1]
PQA-18 (0.1 nM-1 μM) 通过在 Ser141 处自磷酸化以非竞争性和浓度依赖性方式抑制 PAK2 激酶活性 (IC50 为 10 nM,Km 为 2.1 μM)[1]

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

Real Time qPCR[1]

Cell Line: Jurkat cells cultured with ConA
Concentration: 1, 10, 20 μM
Incubation Time: 6 h
Result: Suppressed IL2 mRNA level in ConA-stimulated Jurkat cells.
Affected ∼50% of IL2 transcripts at a high dose (10 μM).
体内研究
(In Vivo)

PQA-18 (0.5 mg/kg,腹腔注射,每周三次) 在 NP-CGG 免疫的 C57BL/6J 小鼠中显示出免疫抑制活性,可抑制调节性 T 细胞亚群的数量和针对 T 细胞依赖性抗原的免疫球蛋白 (Ig) 的产生[1]
PQA-18 软膏 (100 mg/小鼠,含 0.05%-0.1% PQA-18,每周三次,17 周) 可改善 Nc/Nga 小鼠的皮炎和 IgE 水平[1]
QA-18 (1 mg/kg,6周) 对小鼠肝脏和肾脏无明显影响[1]

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

Animal Model: Male C57BL/6J mice (10 weeks old) immunized by intraperitoneal injection of 50 μg NP-CGG[1]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection (i.p.); three times a week
Result: Suppressed the NP-specific responses (IgM, IgG1, and IgG3) in peripheral blood.
Significantly suppressed the number of Foxp3+CD4+CD25+ cells in spleens.
分子量

409.52

Formula

C25H31NO4

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
  • 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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PQA-18
目录号:
HY-171034
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