2. PI3K/Akt/mTOR NF-κB Immunology/Inflammation Apoptosis
  3. PI3K NF-κB Akt NOD-like Receptor (NLR) Pyroptosis Ferroptosis
  4. Sipeimine

Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases.

For research use only. We do not sell to patients.

Sipeimine Chemical Structure

Sipeimine Chemical Structure

CAS No. : 61825-98-7

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Based on 2 publication(s) in Google Scholar

Other Forms of Sipeimine:

Sipeimine Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Akt Akt1 Akt2 Akt3

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NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases[1][2].

In Vitro

Sipeimine (100 μM, 200 μM; 24-48 h) significantly reduces cell viability in mouse chondrocytes[1].
Sipeimine (10-50 μM; 24 h) dose-dependently inhibits lipopolysaccharide (LPS)-induced cytotoxicity in the LDH release assay[1].
Sipeimine (25 μM, 50 μM; 24 h) inhibits the mRNA and protein expression of proinflammatory factors (COX-2, iNOS, IL-1β, IL-18) in 1 μg/mL LPS-induced mouse chondrocytes and reduces PGE2 and nitrite production[1].
Sipeimine (25 μM, 50 μM; 4 h) increases the extracellular matrix components (collagen-II, aggrecan) and reduces the protein expression of degradative enzymes (MMP-13, ADAMTS-5) in mouse chondrocytes in WB experiments[1].
Sipeimine (50 μM; 2-24 h) inhibits LPS-induced NF-κB pathway activation (reduced p-IκBα, p-p65 phosphorylation and p65 nuclear translocation) and NLRP3 inflammasome-mediated cell pyroptosis (reduced NLRP3, ASC, cleaved-caspase-1, cleaved-GSDMD protein expression) in mouse chondrocytes[1].

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

Sipeimine Related Antibodies

RT-PCR[1]

Cell Line: Mouse chondrocytes
Concentration: 0, 25, 50 μM
Incubation Time: 24 h (after LPS stimulation)
Result: Significantly reduced the mRNA levels of pro-inflammatory factors (IL-1β, IL-18, COX-2, iNOS) induced by LPS.

Western Blot Analysis[1]

Cell Line: Mouse chondrocytes
Concentration: 0, 25, 50 μM
Incubation Time: 24 h (after LPS stimulation)
Result: Decreased the protein expressions of COX-2, iNOS, MMP-13, ADAMTS-5, NLRP3, ASC, cleaved-caspase-1, cleaved-GSDMD, p-IκBα, and p-p65, while increased the expressions of collagen-II, aggrecan, and total IκBα, AKT, PI3K.
In Vivo

Sipeimine (30 mg/kg; intra-articular injection; once daily; 14 days) can reduce cartilage degradation, subchondral bone remodeling, synovial inflammation and extracellular matrix (ECM) degradation in the DMM-induced osteoarthritis (OA) mouse model[1].
Sipeimine (15, 30 mg/kg; intraperitoneal injection; once daily; 3 days) can reduce lung tissue damage, pulmonary edema, inflammatory response, inhibit ferroptosis-related indicators (4-HNE, MDA, tissue iron) and upregulate antioxidant factors (GSH, Nrf2, GPX4, HO-1) in the PM2.5-induced lung injury Sprague-Dawley rat model[1].

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

Animal Model: C57BL/6 mice (8-10 weeks old), medial meniscus destabilization (DMM)-induced OA model[1]
Dosage: 30 mg/kg (dissolved in saline with 0.1% DMSO).
Administration: Intra-articular injection, once daily for 14 days, followed by an 8-week observation period.
Result: Significantly reduced subchondral bone volume/tissue volume (BV/TV), trabecular thickness (Tb.Th), and trabecular number (Tb.N), and increased trabecular separation (Tb.Sp) compared to the DMM group.
Histological analysis using Safranin O-fast green and H&E staining showed decreased cartilage degeneration (lower OARSI scores) and synovitis.
Immunohistochemistry revealed reduced expressions of MMP-13, NLRP3, and p-PI3K, and increased collagen-II expression in cartilage tissues.
Animal Model: Male Sprague-Dawley rats (8 weeks old, 110-150 g), PM2.5-induced lung injury model via intratracheal instillation of PM2.5 (7.5 mg/kg/day for 2 days)[2]
Dosage: 15 mg/kg and 30 mg/kg (dissolved in saline with 0.1% DMSO).
Administration: Intraperitoneal injection, once daily for 3 days before PM2.5 exposure.
Result: Dose-dependently alleviated PM2.5-induced lung injury, as indicated by reduced histological scores (thickened alveolar walls, inflammatory cell infiltration, hemorrhage), lower lung wet/dry (W/D) ratio, and decreased levels of TNF-α and IL-1β in bronchoalveolar lavage fluid (BALF).
Reversed PM2.5-induced increases in tissue iron, 4-HNE, and MDA, and restored GSH levels.
Transmission electron microscopy showed attenuated mitochondrial morphological changes (reduced cristae loss and electron density) in type II alveolar epithelial cells.
Western blot revealed upregulated expressions of Nrf2, GPX4, HO-1, SLC7A11, and FTH1, and increased phosphorylation of PI3K and Akt.
Molecular Weight

429.64

Formula

C27H43NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]([C@@]1([H])C2=O)(CC[C@H](O)C1)[C@]3([H])[C@](C2)([H])[C@@](CC[C@]4([H])[C@@]5([H])CN(C[C@@H](C)CC6)[C@]6([H])[C@]4(O)C)([H])[C@@]5([H])C3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (19.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3275 mL 11.6376 mL 23.2753 mL
5 mM 0.4655 mL 2.3275 mL 4.6551 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.77 mg/mL (1.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.77 mg/mL (1.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

SDS (393 KB)

COA (253 KB) HNMR (265 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3275 mL 11.6376 mL 23.2753 mL 58.1882 mL
5 mM 0.4655 mL 2.3275 mL 4.6551 mL 11.6376 mL
10 mM 0.2328 mL 1.1638 mL 2.3275 mL 5.8188 mL
15 mM 0.1552 mL 0.7758 mL 1.5517 mL 3.8792 mL
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Sipeimine Related Classifications

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:

Sipeimine61825-98-7ImperialinePI3KNF-κBAktNOD-like Receptor (NLR)PyroptosisFerroptosisPhosphoinositide 3-kinaseNuclear factor-κBNuclear factor-kappaBPKBProtein kinase BInhibitorinhibitorinhibit

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