| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Biotin-KRpep-2d acetate targets the Ras protein, specifically the K-Ras(G12D) mutant. Ras is a critical member of the Ras protein family and an attractive cancer therapeutic target. The parental KRpep-2d is identified as a selective inhibitory peptide against the K-Ras(G12D) mutant, with selectivity over wild-type (WT) K-Ras and K-Ras(G12C) mutants. This compound is involved in the GPCR/G Protein and MAPK/ERK signaling pathways.
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| ln Vitro |
In vitro, the parental KRpep-2d has demonstrated strong non-covalent inhibition of K-Ras(G12D) in cell-free enzyme activity assays with an IC50 of 1.6 nM. It is also effective in cell-based assays. As a biotinylated derivative, Biotin-KRpep-2d acetate itself is primarily used as a detection tool rather than an active inhibitor in functional assays, enabling the study of K-Ras(G12D) interactions in cellular contexts through streptavidin-based pull-down experiments.
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| ln Vivo |
In vivo activity data for Biotin-KRpep-2d acetate have not been extensively reported in available literature. As a biotin-labeled peptide derivative used primarily as a research tool for affinity purification and detection, its application is predominantly focused on in vitro and ex vivo analyses. Detailed animal model efficacy studies are not typically conducted for this type of labeling reagent.
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| Enzyme Assay |
The assessment of binding affinity for the parental KRpep-2d peptide involves cell-free enzyme activity assays measuring inhibition of K-Ras(G12D). For the biotinylated version, binding studies leverage the high-affinity biotin-streptavidin interaction. The biotin moiety provides strong and specific binding to streptavidin-coated surfaces or beads, allowing for the capture and isolation of K-Ras(G12D) protein complexes from cell lysates or other biological samples.
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| Cell Assay |
Cellular assays for Biotin-KRpep-2d acetate utilize the streptavidin-biotin system for protein interaction studies and detection. The compound can be incubated with cell lysates containing K-Ras proteins, followed by pull-down using streptavidin beads. Bound proteins are then eluted and analyzed by immunoblotting to identify interacting partners. Alternatively, it can be used in immunofluorescence applications to visualize K-Ras localization in fixed cells.
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| Animal Protocol |
Detailed animal experimental protocols for Biotin-KRpep-2d acetate are not described in available literature. The compound is a biotin-labeled research tool intended for use in in vitro biochemical and cell-based assays. In vivo administration studies are not standard for such labeling reagents, and no specific dosing or animal model data are available from product documentation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Biotin-KRpep-2d acetate are not available from standard product literature. As a biotinylated peptide derivative and research reagent, its primary application is in affinity purification and detection assays. Pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion (ADME) are not characterized for this type of tool compound, which is not intended for in vivo therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for Biotin-KRpep-2d acetate have not been extensively reported in standard product literature. As a research-use only compound, routine safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for peptide-based reagents should be followed, including appropriate personal protective equipment.
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| Additional Infomation |
Biotin-KRpep-2d acetate has a molecular weight of 2805.32 with the molecular formula C118H198N46O28S3. The peptide sequence is {Biotin}-Arg-Arg-Arg-Arg-Cys-Pro-Leu-Tyr-Ile-Ser-Tyr-Asp-Pro-Val-Cys-Arg-Arg-Arg-Arg-NH2 with a disulfide bridge between Cys5 and Cys15. The compound is typically stored at -80degC powder for up to 2 years and is soluble in water at 100 mg/mL. It is used exclusively for research purposes and not for human therapy.
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| Molecular Formula |
C118H198N46O28S3
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| Molecular Weight |
2805.32
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| Related CAS # |
KRpep-2d;2098181-84-9
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| Appearance |
White to off-white solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :~100 mg/mL (~35.65 mM)
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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 | 0.3565 mL | 1.7823 mL | 3.5647 mL | |
| 5 mM | 0.0713 mL | 0.3565 mL | 0.7129 mL | |
| 10 mM | 0.0356 mL | 0.1782 mL | 0.3565 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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