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

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.

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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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Description

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)

In Vitro

BChE/p38-α MAPK-IN-1 (Compound 95) shows inhibitory potency against hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM)[1].
BChE/p38-α MAPK-IN-1 (1-5 μM, 18 h) reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) and slightly increases anti-inflammatory cytokine IL-12 in Phytohemagglutinin (PHA) (HY-N7038)-stimulated human peripheral blood mononuclear cells (PBMCs)[1].

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

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.
In Vivo

BChE/p38-α MAPK-IN-1 (Compound 95) (5-10 mg/kg, i.p., 60 min before acquisition trial) improves Scopolamine (HY-N0296)-induced cognitive impairment in adult male Albino Swiss (CD-1) mice[1].
BChE/p38-α MAPK-IN-1 (10 mg/kg, i.p., once daily for 10 days) alleviates LPS (HY-D1056)-induced spatial learning impairment and exerts anti-neuroinflammatory effects in adult male C57BL/6J mice[1].

MedChemExpress (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.
Molecular Weight

454.56

Formula

C26H32F2N4O

CAS No.
SMILES

O=C(C1=CC2=C(C=C1CC3=CC=C(F)C=C3F)C=NN2CC4CCCCC4)NCCN(C)C

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Product Name:
BChE/p38-α MAPK-IN-1
Cat. No.:
HY-175655
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