| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
mSIRK targets the G protein βγ subunits and ERK1/2 signaling pathways. It disrupts the interaction between the α and βγ subunits of G proteins, promoting dissociation of the α subunit. This dissociation activates downstream signaling pathways including ERK1/2, leading to cellular responses.
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|---|---|
| ln Vitro |
mSIRK demonstrates potent in vitro activity as an activator of ERK1/2 with an EC50 of 2.5-5 μM. It is a cell-permeable peptide that can enter cells and activate ERK signaling. The compound disrupts the interaction between G protein α and βγ subunits, promoting α subunit dissociation and downstream ERK activation.
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| ln Vivo |
mSIRK exhibits in vivo activity as an activator of ERK1/2 signaling. As a cell-permeable peptide, it can be administered to animals to study the effects of ERK activation in vivo. The compound may be used to investigate the role of G protein βγ subunits and ERK signaling in various physiological and pathological processes. Comprehensive in vivo studies are needed to fully characterize its efficacy and safety.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for mSIRK involves assessing its ability to disrupt the interaction between G protein α and βγ subunits. Purified G protein subunits are incubated with the peptide, and the dissociation of α and βγ subunits is measured using techniques such as fluorescence polarization, surface plasmon resonance, or size exclusion chromatography. The peptide’s ability to promote α subunit dissociation without stimulating nucleotide exchange is assessed.
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| Cell Assay |
The in vitro cell-based assay for mSIRK involves treating cells with the peptide and measuring ERK1/2 activation. Cells are treated with varying concentrations of mSIRK (EC50 2.5-5 μM), and ERK1/2 phosphorylation is assessed by Western blotting with phospho-specific antibodies. The peptide’s cell-permeable nature allows it to enter cells and activate ERK signaling. Downstream effects on cell proliferation, differentiation, or other ERK-dependent processes may also be measured.
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| Animal Protocol |
In vivo animal experiments for mSIRK involve administering the peptide to animals to study ERK activation in vivo. The peptide is administered via appropriate routes (e.g., intravenous, intraperitoneal), and ERK1/2 phosphorylation is measured in tissues of interest. The compound may be used to investigate the role of G protein βγ subunits and ERK signaling in various physiological and pathological processes.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of mSIRK are not extensively reported. As a 15-amino acid peptide with a cell-permeable sequence， it is expected to have rapid cellular uptake but may be susceptible to proteolytic degradation in vivo. Further pharmacokinetic studies are needed to determine its half-life, bioavailability, and tissue distribution. The compound is typically used for research purposes only.
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| Toxicity/Toxicokinetics |
Toxicological data for mSIRK are not extensively documented. As a research peptide, its safety profile is evaluated in standard cytotoxicity assays. The compound is classified for research use only and is not intended for human therapeutic use. Comprehensive toxicological characterization would be required prior to any clinical development.
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| References | |
| Additional Infomation |
mSIRK (G-Protein βγ Binding Peptide, CAS 593267-11-9) is a cell-permeable activator of ERK1/2 with an EC50 of 2.5-5 μM. It is a 15-amino acid peptide that disrupts G protein α-βγ subunit interaction and promotes α subunit dissociation. It is used in research on G protein signaling and ERK pathways. It is not approved for clinical use and is available only for research purposes. Purity is ≥99.33%.
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| Molecular Formula |
C93H150N20O25
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|---|---|
| Molecular Weight |
1948.305123806
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| Exact Mass |
1947.108
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| CAS # |
593267-11-9
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| PubChem CID |
169450748
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
25
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
69
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| Heavy Atom Count |
138
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| Complexity |
3960
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| Defined Atom Stereocenter Count |
16
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| SMILES |
CCCCCCCCCCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(=O)O)C(=O)O
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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 |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5133 mL | 2.5663 mL | 5.1327 mL | |
| 5 mM | 0.1027 mL | 0.5133 mL | 1.0265 mL | |
| 10 mM | 0.0513 mL | 0.2566 mL | 0.5133 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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