2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Reactive Oxygen Species (ROS) Necroptosis Pyroptosis Interleukin Related
  4. Periplogenin

Periplogenin is a cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis.

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

Periplogenin

Periplogenin Chemical Structure

CAS No. : 514-39-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Periplogenin:

Periplogenin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Periplogenin

View All Interleukin Related Isoform Specific Products:

View All Isoforms
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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Periplogenin is a cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis[1][2][3].

IC50 & Target[2]

IL-1β

 

IL-18

 

Cellular Effect
Cell Line Type Value Description References
HT-1080 IC50
810 nM
Compound: 11
Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
[PMID: 14640513]
In Vitro

Periplogenin (0.625-10 μg/mL 44 h) inhibits the viability of human HaCaT keratinocytes, with an IC50 of 1.56 μg/mL[1].
Periplogenin (2 μg/mL, 6-24 h) induces caspase-independent non-apoptotic and non-autophagic cell death in HaCaT cells[1].
Periplogenin (1-4 μg/mL, 12-48 h) increases ROS production and induces necroptosis in HaCaT cells[1].
Periplogenin (0.1-20 μg/mL, 24 h) inhibits the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS), with an IC50 of 1.56 μg/mL[2].
Periplogenin (0.1-5 μg/mL, 24 h) inhibits the migration, invasion and pyroptosis in RA-FLS[2].
Periplogenin (0.1-5 μg/mL, 24 h) induces G0/G1 phase arrest in RA-FLS[2].
Periplogenin (0.1-5 μg/mL, 24 h) downregulates NLRP3, Cleaved-Caspase-1, GSDMD-N, IL-1β, and IL-18 expression in RA-FLS[2].
Periplogenin (0.02-33 μM, 72 h) inhibits the viability of DU145, DLD-1, U-87MG, and MCF-7 cancer cells, with IC50 values of 2.897 μM, 8.712 μM, 3.008 μM, and 20.025 μM respectively[3].
Periplogenin (0-100 μM) inhibits the enzymatic activity of ATP1A1 in wild-type DU145 cells[3].

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

Periplogenin Related Antibodies

Apoptosis Analysis[1]

Cell Line: HaCaT cells
Concentration: 1, 2 and 4 μg/mL
Incubation Time: 24 and 48 h
Result: Disrupted the membrane integrity.
Increased PI uptake and LDH release.
Revealed necrotic features (cytoplasmic swelling, reduced organelles, nuclear membrane disorder).

Cell Cycle Analysis[2]

Cell Line: RA-FLS
Concentration: 0.1, 0.5 and 5 μg/mL
Incubation Time: 24 h
Result: Increased the proportion of G0/G1 phase cells.
Decreased the proportion of G2/M phase cells.
Showed no significant change in S phase cell proportion.
In Vivo

Periplogenin (2 μg per site, topical application, daily for 11 days starting after 8 days of TPA induction) ameliorates TPA-induced and IMQ (HY-B0180)-induced psoriasis-like skin inflammation in Balb/c mice[1].
Periplogenin (10-20 mg/kg, i.g., once a day) inhibits tumor growth in DU145 wild-type xenograft mice models[3].

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

Animal Model: TPA-induced and IMQ (HY-B0180)-induced psoriasis-like mice models[1]
Dosage: 2 μg per site
Administration: Topical application, daily for 11 days starting after 8 days of TPA induction
Result: Reduced ear thickness and weight.
Alleviated epidermal hyperplasia and inflammatory cell infiltration in dorsal skin and ears.
Animal Model: DU145 wild-type xenograft mice models[3]
Dosage: 10 and 20 mg/kg
Administration: Orally gavage, once a day
Result: Reduced tumor volume and weight.
Had no significant change in body weight.
Molecular Weight

390.51

Formula

C23H34O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]12[C@@]3([H])[C@@](CC[C@@]1([C@@H](C4=CC(OC4)=O)CC2)C)([H])[C@@]5([C@@](O)(C[C@@H](O)CC5)CC3)C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (256.08 mM; Need ultrasonic; 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 2.5608 mL 12.8038 mL 25.6075 mL
5 mM 0.5122 mL 2.5608 mL 5.1215 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (6.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.91%

SDS (251 KB)

COA (257 KB) HNMR (202 KB) CNMR (180 KB) RP-HPLC (343 KB) MS (520 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5608 mL 12.8038 mL 25.6075 mL 64.0188 mL
5 mM 0.5122 mL 2.5608 mL 5.1215 mL 12.8038 mL
10 mM 0.2561 mL 1.2804 mL 2.5608 mL 6.4019 mL
15 mM 0.1707 mL 0.8536 mL 1.7072 mL 4.2679 mL
20 mM 0.1280 mL 0.6402 mL 1.2804 mL 3.2009 mL
25 mM 0.1024 mL 0.5122 mL 1.0243 mL 2.5608 mL
30 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1340 mL
40 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6005 mL
50 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2804 mL
60 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
80 mM 0.0320 mL 0.1600 mL 0.3201 mL 0.8002 mL
100 mM 0.0256 mL 0.1280 mL 0.2561 mL 0.6402 mL
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Periplogenin 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:

Periplogenin514-39-6Reactive Oxygen Species (ROS)NecroptosisPyroptosisInterleukin RelatedILCardiac glycosideCortex periplocaeROSNLRP3/Caspase-1/GSDMDATP1A1Prostate carcinomaRheumatoid arthritisPsoriasisInhibitorinhibitorinhibit

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