| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Von Hippel-Lindau (VHL) protein (as an inactive control ligand).
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|---|---|
| ln Vitro |
(S,S,S)-AHPC-Boc is the inactive isomer of (S,R,S)-AHPC-Boc and is used as a negative control compound in experiments. Unlike its active stereoisomer, it does not functionally recruit VHL proteins for targeted protein degradation. It is used as a comparator or baseline control in PROTAC studies where stereochemistry is relevant. The compound allows researchers to distinguish between specific VHL-mediated effects and non-specific effects in PROTAC experiments.
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| ln Vivo |
(S,S,S)-AHPC-Boc is not designed for in vivo activity as it is an inactive control compound. It is used as a negative control in experiments to establish baseline activity and rule out non-specific effects. In vivo studies of the active isomer (S,R,S)-AHPC-Boc in PROTAC applications involve administration to animal models to evaluate targeted protein degradation, but the (S,S,S) isomer serves only as a control.
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| Enzyme Assay |
Non-cell-based assays for VHL ligand binding typically involve surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure binding affinity between the VHL ligand and the VHL protein. Competitive binding assays using fluorescence polarization (FP) or AlphaScreen technology can be employed to evaluate the displacement of a labeled VHL ligand by test compounds. The (S,S,S) isomer is used as a negative control to confirm the specificity of binding interactions observed with the active (S,R,S) isomer.
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| Cell Assay |
For cell-based studies, cells are treated with PROTAC molecules containing the active VHL ligand (S,R,S)-AHPC-Boc, with the (S,S,S) isomer used as a control. Cells are cultured in appropriate medium and treated with compounds at various concentrations for 24-72 hours. Target protein levels are assessed by Western blot or immunofluorescence. The (S,S,S) control helps confirm that protein degradation is specifically mediated by VHL recruitment and not by off-target effects.
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| Animal Protocol |
In vivo studies using the active VHL ligand (S,R,S)-AHPC-Boc in PROTAC applications involve administration to animal models (typically mice) via intravenous or intraperitoneal injection. The (S,S,S) isomer serves as a negative control. Pharmacodynamic endpoints include measurement of target protein degradation in tissues by Western blot or ELISA. Pharmacokinetic parameters are assessed from plasma and tissue samples collected at various time points.
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| ADME/Pharmacokinetics |
As a control compound used primarily in vitro, detailed pharmacokinetic data for (S,S,S)-AHPC-Boc are limited. The active isomer (S,R,S)-AHPC-Boc (VH032-Boc) is a small molecule VHL ligand with moderate molecular weight (530.68 g/mol). It is soluble in DMSO (50 mg/mL) and can be formulated for in vivo administration using DMSO/PEG300/Tween 80/saline or DMSO/corn oil mixtures. The compound should be stored in a sealed, protected environment (e.g., under nitrogen) to avoid moisture exposure.
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| Toxicity/Toxicokinetics |
As an inactive control compound, (S,S,S)-AHPC-Boc is not expected to exhibit significant toxicity. It is used in laboratory research at low concentrations and should be handled with standard laboratory safety practices. The active VHL ligand (S,R,S)-AHPC-Boc has been used in preclinical studies with acceptable safety profiles. No specific toxicity data are available for the (S,S,S) isomer. Standard precautions for handling chemical research compounds should be followed.
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| References | |
| Additional Infomation |
(S,S,S)-AHPC-Boc is a critical tool compound for PROTAC research. PROTACs are heterobifunctional molecules that recruit E3 ubiquitin ligases (such as VHL) to target proteins for ubiquitination and subsequent proteasomal degradation. The (S,S,S) isomer serves as an essential negative control to validate that observed degradation effects are due to specific VHL recruitment and not non-specific mechanisms. This compound is for research use only and is not intended for therapeutic applications.
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| Molecular Formula |
C27H38N4O5S
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|---|---|
| Molecular Weight |
530.68
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| CAS # |
1797406-74-6
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| Related CAS # |
(S,R,S)-AHPC-Boc;1448189-98-7
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| Appearance |
Light yellow to green yellow 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. |
| 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) |
DMSO: 50 mg/mL (94.22 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 | 1.8844 mL | 9.4219 mL | 18.8437 mL | |
| 5 mM | 0.3769 mL | 1.8844 mL | 3.7687 mL | |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8844 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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