2. MAPK/ERK Pathway Neuronal Signaling Immunology/Inflammation
  3. p38 MAPK Cholinesterase (ChE) Interleukin Related
  4. BChE/p38-α MAPK-IN-1

BChE/p38-α MAPK-IN-1 是一种选择性的双重抑制剂，针对 hBChE (IC50 = 772 nM) 和 p38α MAPK (IC50 = 191 nM)。BChE/p38-α MAPK-IN-1 可减少细胞中促炎性细胞因子 (IL-1β、IL-6、IL-8、TNF-α) 的产生。BChE/p38-α MAPK-IN-1 能够改善 Scopolamine (HY-N0296) 诱导的认知障碍，同时缓解 LPS (HY-D1056) 诱导的空间学习障碍，并在小鼠中发挥抗神经炎症作用。BChE/p38-α MAPK-IN-1 可用于阿尔茨海默病 (AD) 的研究。

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BChE/p38-α MAPK-IN-1

BChE/p38-α MAPK-IN-1 Chemical Structure

CAS No. : 3077831-11-6

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BChE/p38-α MAPK-IN-1 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BChE/p38-α MAPK-IN-1 is a selective dual inhibitor of hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). BChE/p38-α MAPK-IN-1 reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells. BChE/p38-α MAPK-IN-1 improves Scopolamine (HY-N0296)-induced cognitive impairment, as well as alleviates LPS (HY-D1056)-induced spatial learning impairment and exerts anti-neuroinflammatory effects in mice. BChE/p38-α MAPK-IN-1 can be used for the study of Alzheimer’s disease (AD) by targeting both cholinergic deficit and neuroinflammation[1].

IC50 & Target[1]

p38α MAPK

191 nM (IC50)

hBCHE

772 nM (IC50)

体外研究
(In Vitro)

BChE/p38-α MAPK-IN-1 (Compound 95) 对 hBChE (IC50 = 772 nM) 和 p38α MAPK (IC50 = 191 nM) 表现出抑制活性[1]。
BChE/p38-α MAPK-IN-1 (1-5 μM, 18 h) 在植物血凝素 (PHA) (HY-N7038) 刺激的人外周血单核细胞 (PBMCs) 中减少促炎性细胞因子 (IL-1β, IL-6, IL-8, TNF-α) 的产生，并略微增加抗炎性细胞因子 IL-12[1]。

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

BChE/p38-α MAPK-IN-1 相关抗体:

ELISA Assay[1]

Cell Line: Phytohemagglutinin (PHA) (HY-N7038)-stimulated human peripheral blood mononuclear cells (PBMCs)
Concentration: 1, 2.5, 5 μM
Incubation Time: 18 h
Result: Reduced the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) and slightly increases anti-inflammatory cytokine IL-12.
体内研究
(In Vivo)

BChE/p38-α MAPK-IN-1 (Compound 95) (5-10 mg/kg， 腹腔注射， 在试验前 60 分钟) 改善成年雄性白化瑞士 (CD-1) 小鼠中 Scopolamine (HY-N0296) 诱导的认知障碍[1]。
BChE/p38-α MAPK-IN-1 (10 mg/kg， 腹腔注射， 每天一次，持续 10 天) 缓解成年雄性 C57BL/6J 小鼠中 LPS (HY-D1056) 诱导的空间学习障碍，并发挥抗神经炎症作用[1]。

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

Animal Model: Adult male Albino Swiss (CD-1) mice were subcutaneously injected with scopolamine (1 mg/kg) 30 min before the acquisition trial of passive avoidance (PA) and novel object recognition (NOR) tasks to induce cholinergic deficit-related cognitive impairment[1]
Dosage: 5, 10 mg/kg
Administration: i.p., 60 min before acquisition trial
Result: Prolonged the step-through latency of mice in the memory retention trial at a dose of 10 mg/kg.
Improved scopolamine-induced long-term contextual memory impairment.
Increased the discrimination index of mice at a dose of 10 mg/kg.
Animal Model: Adult male C57BL/6J mice were intraperitoneally injected with LPS at doses of 2.5 mg/kg (2 days), 2 mg/kg (2 days), and 1.5 mg/kg (2 days) respectively[1]
Dosage: 10 mg/kg
Administration: i.p., once daily for 10 days
Result: Reduced the escape latency of mice in morris water maze spatial learning task.
Reduced the expression levels of inflammation-related proteins (TLR4, COX-2, and NLRP3) in mouse brains.
Had no obvious effect on the expression of cPLA2 protein.
分子量

454.56

Formula

C26H32F2N4O
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

BChE/p38-α MAPK-IN-1 相关分类

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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:

BChE/p38-α MAPK-IN-13077831-11-6p38 MAPKCholinesterase (ChE)Interleukin RelatedILhBChEp38-α MAPKAlzheimer’s disease (AD)neuroinflammationpro-inflammatory cytokinesInhibitorinhibitorinhibit

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