Mastoparan |
Catalog No.GC12692
One-Click Copy Product Info
|
Mastoparan, a peptide toxin from wasp venom, induces stimulation of phosphoinositide breakdown with an EC50 value of 9μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 72093-21-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Mastoparan, a peptide toxin from wasp venom, induces stimulation of phosphoinositide breakdown with an EC50 value of 9μM[1]. Mastoparan accelerates guanosine-5'-3-O-thiotriphosphate binding and consequent GTP-binding regulatory protein (G protein) activation in part by enhancing the dissociation of bound GDP[2]. Mastoparan has been widely used in anti-inflammatory studies and as a model compound to develop related derivatives[3].
In vitro, Mastoparan exhibited an anticancer towards Hep-G2 cells with IC50=189.59±0.6µg/ml after 24h treatment[4]. Treatment with 25μM Mastoparan for 8h significantly induced cell death in Jurkat T leukemia cells and normal peripheral blood cells[5]. Mastoparan treatment at 20μM within 1min significantly induced a rapid increase in cytosolic-free Ca2+ concentration elevation in Tobacco BY-2 cells[6].
In vivo, Mastoparan treatment via a peritumor route at 5 mg/kg/day for 5 consecutive days inhibited the tumor growth in the murine melanoma model[7]. The combination therapy of gemcitabine (60mg/kg/day) and Mastoparan (6mg/kg/day) for 14 days via intraperitoneal injection significantly inhibited tumor progression in a mouse model of breast cancer[5].
References:
[1] Gusovsky F, Soergel D G, Daly J W. Effects of mastoparan and related peptides on phosphoinositide breakdown in HL-60 cells and cell-free preparations[J]. European Journal of Pharmacology: Molecular Pharmacology, 1991, 206(4): 309-314.
[2] Higashijima T, Uzu S, Nakajima T, et al. Mastoparan, a peptide toxin from wasp venom, mimics receptors by activating GTP-binding regulatory proteins (G proteins)[J]. Journal of Biological Chemistry, 1988, 263(14): 6491-6494.
[3] Chen X, Zhang L, Wu Y, et al. Evaluation of the bioactivity of a mastoparan peptide from wasp venom and of its analogues designed through targeted engineering[J]. International journal of biological sciences, 2018, 14(6): 599.
[4] Elsharkawy A M, Galhom R A, Amin B H, et al. In Vitro Evaluation of Some Therapeutic Applications of Wasp Venom and Mastoparan[J]. Egyptian Academic Journal of Biological Sciences. A, Entomology, 2024, 17(1): 121-130.
[5] Hilchie A L, Sharon A J, Haney E F, et al. Mastoparan is a membranolytic anti-cancer peptide that works synergistically with gemcitabine in a mouse model of mammary carcinoma[J]. Biochimica Et Biophysica Acta (BBA)-Biomembranes, 2016, 1858(12): 3195-3204.
[6] Takahashi K, Isobe M, Muto S. Mastoparan induces an increase in cytosolic calcium ion concentration and subsequent activation of protein kinases in tobacco suspension culture cells[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 1998, 1401(3): 339-346.
[7] de Azevedo R A, Figueiredo C R, Ferreira A K, et al. Mastoparan induces apoptosis in B16F10-Nex2 melanoma cells via the intrinsic mitochondrial pathway and displays antitumor activity in vivo[J]. Peptides, 2015, 68: 113-119.
| Cell experiment [1]: | |
|
Cell lines |
Immortalized human dermal microvessel endothelial cells |
|
Preparation Method |
The growth of immortalized human dermal microvessel endothelial cells (HMECs) occurred in MCDB-131 medium which contained 10% inactivated FBS and 2mM glutamine as well as 100U/ml penicillin and 100μg/ml streptomycin. HMECs were seeded in 24-well culture plates (approximate cell density, 3×105 cells/well) containing medium supplemented with 5% heat-inactivated FBS. After cells reached confluence, cells were stimulated for 6h with lipopolysaccharide (LPS) at 10ng/ml, with or without a 30min preincubation of cells with Mastoparan (0, 5, 10, 15, 20, and 25μM). Supernatants were harvested and assayed for IL-6 activity by ELISA. |
|
Reaction Conditions |
0, 5, 10, 15, 20, and 25μM; 30min |
|
Applications |
Mastoparan exerted a dose-dependent inhibition on the expression and secretion of IL-6 induced by LPS. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6 mice |
|
Preparation Method |
At 6 to 8 weeks of age of male C57BL/6 mice, 5×104 viable B16F10-Nex2 cells were subcutaneously (s.c.) inoculated on the right side of male C57BL/6 mice. When the tumor reached a volume of 100mm3, the mice received 5 weekly intratumoral doses of Mastoparan (5mg/kg/day). The untreated tumor control group received 100μL PBS. After administration of the therapeutic dose, the tumor size was measured daily using a caliper. The tumor volume (V) was calculated using the formula V=0.52×d2×D, where d and D are the short and long diameters of the tumor, respectively. When the tumor size reached a maximum of 3000mm3, the animals were sacrificed for subsequent experimental analysis. |
|
Dosage form |
5mg/kg/day for 5 weeks a day; i.t. |
|
Applications |
Mastoparan treatment inhibited the growth of subcutaneous melanoma in mice and increased the survival rate. |
|
References: |
|
| Cas No. | 72093-21-1 | SDF | |
| Chemical Name | (S,Z)-2-((Z)-((2S,3S)-2-amino-1-hydroxy-3-methylpentylidene)amino)-N'1-((4S,5Z,7S,8Z,10S,11Z,13S,14Z,16S,17Z,19S,20Z,22S,23Z,25S,26Z,28S,29Z,31S,32Z,34S,35Z,37S)-10,13,34-tris(4-aminobutyl)-7-((S)-sec-butyl)-6,9,12,15,18,21,24,27,30,33,36-undecahydroxy-4- | ||
| Canonical SMILES | CC[C@]([C@@](N)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC(C)C)([H])[C@@](CC)([H])C)([H])CCCCN)([ | ||
| Formula | C70H131N19O15 | M.Wt | 1479 |
| Solubility | Soluble to 2.60 mg/ml in sterile water | Storage | Desiccate at -20°C |
| 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. |
||
| 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 | 676.1 μL | 3.3807 mL | 6.7613 mL |
| 5 mM | 135.2 μL | 676.1 μL | 1.3523 mL |
| 10 mM | 67.6 μL | 338.1 μL | 676.1 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 1 reference(s) in Google Scholar.)