Periplocin |
Catalog No.GC44600
One-Click Copy Product Info
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Periplocin is one of the cardenolides isolated from Periploca sepium, with anti-proliferative activities.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13137-64-9
Sample solution is provided at 25 µL, 10mM.
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Periplocin is one of the cardenolides isolated from Periploca sepium, with anti-proliferative activities[1]. Periplocin can increase the caspase-3, -8, and -9 enzyme activities and decrease PI3K/Akt/mTOR activity to trigger apoptosis[2]. Periplocin has been widely used as an anticancer agent in cellular and animal models to inhibit cancer progression[3].
In vitro, Periplocin treatment significantly inhibited the proliferation of Muc-Myx2a, Muc-Myx2b and T60 cells with IC50 values of 0.25µM, 0.30µM, and 0.10µM, respectively[4]. Periplocin treatment at 50µM for 24 hours significantly activated RIP3/MLKL signaling pathway and induced necroptosis in TPC-1 cells[5]. Treatment of SK-HEP-1 cells with 500nM Periplocin for 48 hours significantly induced cell cycle arrest and apoptosis, accompanied by the inhibition of AKT/NF-κB signaling pathway[6].
In vivo, Periplocin treatment via intraperitoneal injection at a dose of 15mg/kg/day for 14 days notably reduced tumor growth in A549 cell-xenograft mice and decreased Ki67 expression in the tumor tissues[7]. Daily intraperitoneal injection of Periplocin at a dose of 5mg/kg for 8 weeks reduced bone loss in ovariectomy-induced osteoporotic mice[8].
References:
[1] Lohberger B, Wagner S, Wohlmuther J, et al. Periplocin, the most anti-proliferative constituent of Periploca sepium, specifically kills liposarcoma cells by death receptor mediated apoptosis[J]. Phytomedicine, 2018, 51: 162-170.
[2] Liu X, Liu J, Yan B, et al. Study of the PI3K/Akt/mTOR signaling pathway in vitro and molecular docking analysis of periplocin inhibits cell cycle progression and induces apoptosis in MDA‐MB‐231[J]. Environmental Toxicology, 2024, 39(1): 444-456.
[3] Bae E S, Byun W S, Ock C W, et al. Periplocin exerts antitumor activity by regulating Nrf2-mediated signaling pathway in gemcitabine-resistant pancreatic cancer cells[J]. Biomedicine & Pharmacotherapy, 2023, 157: 114039.
[4] Lohberger B, Bernhart E, Stuendl N, et al. Periplocin mediates TRAIL-induced apoptosis and cell cycle arrest in human myxofibrosarcoma cells via the ERK/p38/JNK pathway[J]. Phytomedicine, 2020, 76: 153262.
[5] Ding L, Wen F, Zeng L, et al. Periplocin induces necroptosis in papillary thyroid carcinoma through DR4 mediated RIPK3 and MLKL signaling[J]. Scientific Reports, 2025, 15(1): 20383.
[6] Lin J P, Huang M H, Sun Z T, et al. Periplocin inhibits hepatocellular carcinoma progression and reduces the recruitment of MDSCs through AKT/NF-κB pathway[J]. Life Sciences, 2023, 324: 121715.
[7] Wang J, Zhu Y, Song J, et al. Periplocin potentiates ferroptotic cell death in non-small cell lung cancer by inducing the degradation of Nrf2[J]. Cancer Cell International, 2025, 25(1): 294.
[8] Zhang X, Sun Z, Zhang Y, et al. Periplocin targets low density lipoprotein receptor-related protein 4 to attenuate osteoclastogenesis and protect against osteoporosis[J]. Biochemical Pharmacology, 2023, 211: 115516.
| Cell experiment [1]: | |
Cell lines | TPC-1 cells |
Preparation Method | TPC-1 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 100U/ml streptomycin. The culture conditions were 37℃ and 5% CO2 in a humidified incubator. TPC-1 cells were seeded in 96-well plates at a density of 2000 cells per well and treated with various concentrations of Periplocin (62.5nM, 125nM, 250nM, and 500nM) for 48h, CCK-8 reagent was added, and absorbance was measured at 450nm. |
Reaction Conditions | 62.5nM, 125nM, 250nM, and 500nM; 48h |
Applications | Periplocin treatment significantly inhibited the viability of TPC-1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Six-week-old female nude mice were raised in a standard sterile environment, and 1×106 A549 cells were suspended in 100µl PBS and injected subcutaneously into the mice. When the tumor volume reached approximately 50mm3, the mice were randomly divided into three groups and received intraperitoneal injection of vehicle (5% DMSO, 10% ethanol, and 85% saline), Periplocin (15mg/kg/day), or imidazole ketone erastin (IKE) (40mg/kg/day) for two weeks. The tumor size was measured using a vernier caliper every two days. And calculate the tumor volume via the formula: (length×width2)×(1/2). |
Dosage form | 15mg/kg/day for 14 days; i.p. |
Applications | Periplocin treatment markedly reduced tumor growth in A549 cell-xenograft mice. |
References: | |
| Cas No. | 13137-64-9 | SDF | |
| Canonical SMILES | C[C@@]12[C@@](CC[C@@H]2C(CO3)=CC3=O)(O)[C@]4([H])CC[C@]5(O)C[C@@H](O[C@]6([H])O[C@H](C)[C@@H](O[C@@]7([H])[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O7)[C@@H](OC)C6)CC[C@]5(C)[C@@]4([H])CC1 | ||
| Formula | C36H56O13 | M.Wt | 696.8 |
| Solubility | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4351 mL | 7.1757 mL | 14.3513 mL |
| 5 mM | 287 μL | 1.4351 mL | 2.8703 mL |
| 10 mM | 143.5 μL | 717.6 μL | 1.4351 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)