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| Targets |
Hsp90 (heat shock protein 90)-survivin complex. Shepherdin (79-87) acts as an inhibitor of the survivin-heat shock protein 90 (Hsp90) interaction, binding to the N-terminal domain of Hsp90 in a concentration-dependent manner. At 150 uM, it inhibits the interaction between recombinant human survivin and Hsp90 in isolated human reticulocyte extracts.
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| ln Vitro |
In vitro, Shepherdin (79-87) TFA functions as an inhibitor of the survivin-Hsp90 interaction. It binds to the N-terminal domain of Hsp90 in a concentration-dependent manner and at 150 uM inhibits the interaction between recombinant human survivin and Hsp90 in isolated human reticulocyte extracts. Conjugates of Shepherdin with cell-penetrating peptides (penetratin or HIV Tat sequence) exhibit anticancer properties both in vitro and in vivo.
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| ln Vivo |
In vivo, Shepherdin conjugates with cell-permeable peptides (penetratin or HIV Tat sequence) show anticancer activity. The cell-penetrating peptide conjugation enables intracellular delivery of Shepherdin (79-87), allowing it to disrupt the survivin-Hsp90 complex within cancer cells. This leads to reduced survivin stability, increased apoptosis, and decreased tumor growth in preclinical cancer models.
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| Enzyme Assay |
Survivin-Hsp90 interaction inhibition assay: Recombinant human survivin is incubated with His-tagged Hsp90 (N-terminal domain) in binding buffer (20 mM HEPES pH 7.4, 50 mM KCl, 5 mM MgCl2, 1 mM ATP) with increasing concentrations of Shepherdin (79-87) TFA (0-500 uM) for 60 min at 4degC. The complexes are pulled down using Ni-NTA beads and washed. Bound survivin is detected by Western blotting using anti-survivin antibody. The inhibition concentration (150 uM) is determined by densitometry.
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| Cell Assay |
Cell viability and apoptosis assay protocol: Cancer cells (e.g., HeLa, MCF-7, or PC-3) are seeded in 96-well plates (5,000-10,000 cells/well). Shepherdin (79-87) TFA is conjugated to cell-penetrating peptides (e.g., penetratin) prior to treatment. Cells are treated with conjugated Shepherdin at concentrations of 0-200 uM for 48 hours. Cell viability is assessed by MTT assay. Apoptosis is measured by flow cytometry using Annexin V-FITC/PI staining or by caspase-3/7 activity assay.
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| Animal Protocol |
Xenograft tumor model protocol (example): Female BALB/c nude mice (6-8 weeks old) are subcutaneously implanted with cancer cells (5×10⁶ cells/mouse). When tumors reach ~100-150 mm3, mice are randomized into groups (n=6-8). Shepherdin conjugated to cell-penetrating peptide (e.g., penetratin or Tat) is administered via intraperitoneal injection or tail vein injection at doses of 10-50 mg/kg, daily or every other day for 14-21 days. Tumor volume is measured every 2-3 days with calipers. Tumors are collected for survivin and Hsp90 co-immunoprecipitation, Western blotting, and TUNEL staining.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Shepherdin (79-87) TFA are limited. As a peptide (MW 949.10, TFA salt form), the compound has limited stability in circulation due to proteolytic degradation. Conjugation to cell-penetrating peptides (e.g., penetratin) may enhance cellular uptake but does not significantly extend plasma half-life. For in vivo studies, peptides are typically administered via intraperitoneal or intravenous routes. Storage at -20degC to -80degC is recommended.
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| Toxicity/Toxicokinetics |
Toxicity data for Shepherdin (79-87) TFA are limited. The peptide is intended for research use only and not for human therapeutic applications. As an inhibitor of the survivin-Hsp90 interaction, it may affect normal proliferating tissues since survivin is also expressed in certain normal cells. Conjugation with cell-penetrating peptides may enhance delivery but could also increase non-specific toxicity. Standard safety precautions should be observed.
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| References | |
| Additional Infomation |
Shepherdin (79-87) TFA is a research tool peptide for studying survivin-Hsp90 protein-protein interactions. Survivin is a key regulator of tumor cell viability and an important anticancer target. The peptide is derived from the survivin protein sequence that interacts with Hsp90. The TFA salt form is used to enhance peptide stability and solubility. Shepherdin has not entered clinical trials and is not approved for human use. The sequence is Lys-His-Ser-Ser-Gly-Cys-Ala-Phe-Leu-OH (MW 949.10).
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| Molecular Formula |
C43H65F3N12O14S
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| Molecular Weight |
1063.11
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| Related CAS # |
Shepherdin (79-87);861224-28-4
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| Appearance |
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 :≥ 70 mg/mL (~65.84 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 | 0.9406 mL | 4.7032 mL | 9.4064 mL | |
| 5 mM | 0.1881 mL | 0.9406 mL | 1.8813 mL | |
| 10 mM | 0.0941 mL | 0.4703 mL | 0.9406 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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