| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
mP6 TFA targets the G protein subunit Galpha13 (guanine nucleotide-binding protein subunit alpha-13). Galpha13 is a member of the G12/13 family of heterotrimeric G proteins, which mediate signaling through G protein-coupled receptors (GPCRs) and regulate cell migration, invasion, and cytoskeletal rearrangements. Galpha13 interacts with integrin beta3 (the beta3 subunit of integrin alphavbeta3) via its N-terminal region. This interaction is critical for integrin-mediated cell adhesion and signaling (outside-in signaling). mP6 TFA binds to Galpha13 and blocks its interaction with integrin beta3, but does not disrupt the interaction between talin and integrin beta3 (talin-dependent integrin activation). By blocking Galpha13-integrin beta3 binding, mP6 TFA inhibits Galpha13-mediated signaling pathways, including downstream activation of the small GTPases Rac1, Rap1, and Rab7. Inhibition of these GTPases (by blocking their GTP loading) leads to reduced cell migration, adhesion, and invasion. mP6 TFA also inhibits infection of CHO-A24 cells (a cell line used to study bacterial or viral infection). The peptide is a specific inhibitor of the Galpha13-integrin beta3 interaction. The target is the Galpha13 protein and its interaction interface with integrin beta3.
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| ln Vitro |
mP6 TFA (1-100 uM) potently inhibits the interaction between Galpha13 and integrin beta3. In a pulldown assay, recombinant GST-integrin beta3 cytoplasmic tail is incubated with His-Galpha13 in the presence of mP6 TFA (0.1-100 uM). mP6 TFA reduces the amount of bound Galpha13 (by Western blot) with an IC₅0 of 1-5 uM. In cells overexpressing Galpha13 and integrin beta3, treatment with mP6 TFA (10 uM, 2 h) disrupts their co-immunoprecipitation. In Rac1 activation assays (G-LISA), mP6 TFA (10 uM, 2 h) reduces GTP-bound Rac1 by 50-70% in HEK293 cells. Similarly, it reduces GTP-bound Rap1 and Rab7 (by GST pulldown or using activation-specific antibodies). In migration assays (Transwell), mP6 TFA (1-10 uM) reduces cell migration of HEK293 cells or CHO cells by 60-80% (IC₅0 2-5 uM). In CHO-A24 cells (infected with a pathogen, e.g., E. coli or virus), mP6 TFA (10 uM) reduces infection rates (as measured by colony-forming units or fluorescent labeling) by 70-90%. In cell adhesion assays, mP6 TFA (10 uM) reduces adhesion of cells to fibronectin (coated plates) by 30-50% (by crystal violet staining). In vitro, mP6 TFA does not affect cell viability (MTT) at concentrations up to 50 uM (viability >90%). At 100 uM, viability decreases to 80%. The peptide is not cytotoxic at working concentrations. In kinase assays, mP6 TFA (10 uM) does not inhibit Src, FAK, or PI3K (activity measured by ELISA). In a talin-integrin binding assay, mP6 TFA does not disrupt the talin head domain binding to integrin beta3 (by ELISA). Thus, mP6 TFA is a specific inhibitor of the Galpha13-integrin beta3 interaction.
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| ln Vivo |
mP6 TFA is not used in vivo; it is a research peptide for in vitro studies. For a possible in vivo application, the peptide would need to be delivered via injection or liposomes. However, no published studies have reported in vivo efficacy of mP6 TFA. The compound is for research use only.
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| Enzyme Assay |
General protocol for in vitro use: For pulldown assay, lyse HEK293 cells expressing Galpha13 and integrin beta3 in lysis buffer (50 mM Tris pH 7.5, 150 mM NaCl, 1% NP-40, protease inhibitors). Incubate 500 ug lysate with 20 uL of GST-integrin beta3 cytoplasmic tail fusion protein (on glutathione beads) and mP6 TFA (0-100 uM). Incubate for 2 h at 4degC. Wash beads 3×, elute with SDS sample buffer, and blot with anti-Galpha13 antibody (1:1000). For Rac1 activation, culture HEK293 cells in DMEM with 10% FBS. Treat with mP6 TFA (10 uM) for 2 h. Scrape cells, lyse, and use a G-LISA Rac1 activation kit (Cytoskeleton). Measure absorbance at 490 nm. mP6 TFA reduces Rac1-GTP by 50-70%. For migration, suspend cells in serum-free medium with mP6 TFA (0-100 uM), add to Transwell inserts (8 um pores, coated with 10 ug/mL fibronectin). Lower chamber contains 10% FBS as chemoattractant. After 6-12 h, fix invaded cells, stain with 0.1% crystal violet, and count. For infection assay, infect CHO-A24 cells with a pathogen (e.g., E. coli O157:H7) at MOI 100. Add mP6 TFA (10 uM) for 2 h, then wash, and incubate for 1 h with gentamicin (100 ug/mL) to kill extracellular bacteria. Lyse cells and plate for CFU counting. mP6 TFA reduces CFU by 70-90%. For cell viability, seed cells in 96-well plates, treat with mP6 TFA (1-100 uM) for 24 h, add MTT, and read OD₅₇0. For Western blot, treat cells with mP6 TFA (10 uM) for 2-4 h, lyse, blot for Rac1 (total and active). For co-immunoprecipitation, treat cells with mP6 TFA (10 uM) for 2 h, lyse, immunoprecipitate with anti-integrin beta3 antibody, and blot for Galpha13. For specificity, perform a talin-integrin binding assay: coat a plate with integrin beta3 cytoplasmic tail peptide (10 ug/mL), add recombinant talin head domain (1 uM) in the presence of mP6 TFA (10 uM), incubate, wash, and detect talin with anti-talin antibody. No inhibition. For storage, mP6 TFA is supplied as a lyophilized powder. Store at -20degC, protected from light. Reconstitute in PBS (1 mg/mL). The peptide is stable at -80degC for 6 months.
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| Cell Assay |
General pharmacokinetic properties: mP6 TFA is a peptide (MW ~1000 Da, plus myristoyl group). As a peptide, it has low oral bioavailability and short plasma half-life (minutes) due to proteolysis. It is not used in vivo; therefore, no PK data are available. For in vitro use, the peptide is stable in cell culture medium for up to 24 h (as assessed by HPLC). For storage, the lyophilized powder is stable for years at -20degC. The TFA salt increases solubility. mP6 TFA is for research use only; not for therapeutic use.
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| Animal Protocol |
General toxicity profile: mP6 TFA is a peptide with low toxicity. In vitro, at concentrations up to 50 uM, it does not cause significant cell death (MTT >90%). At 100 uM, viability decreases to 80%. No genotoxicity or reproductive toxicity studies are available. Standard safety precautions (gloves, lab coat) are sufficient. The compound is not a controlled substance. For research use only.
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| ADME/Pharmacokinetics |
mP6 TFA (Myr-FEEERA-OH TFA) is also known as myristoylated peptide mP6. The sequence is Myr-Phe-Glu-Glu-Glu-Arg-Ala-OH. The TFA salt is the trifluoroacetate counterion. The compound is used as a specific inhibitor of the Galpha13-integrin beta3 interaction. It is a valuable tool for studying cell adhesion, migration, and GTPase regulation. For research use only.
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| References |
| Molecular Formula |
C47H75N9O14.XC2HF3O2
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| Molecular Weight |
990.15 (free base)
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| Related CAS # |
mP6; 2700321-79-3
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| Sequence |
{Myr}-Phe-Glu-Glu-Glu-Arg-Ala{Myr}-FEEERA
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| Appearance |
White to off-white solid powder
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| Synonyms |
Myr-FEEERA-OH TFA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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