| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PhosTAC5 does not target a specific enzyme or receptor directly; rather, it acts as a molecular bridge. It contains two key components: (1) a ligand that binds to a target protein of interest (PDCD4 or FOXO3a), and (2) a ligand that recruits a protein phosphatase (presumably PP1, PP2A, or another serine/threonine phosphatase). Upon binding to both the target and the phosphatase simultaneously, PhosTAC5 brings the phosphatase into close proximity with the target protein, facilitating its dephosphorylation. The PEG linker of five units provides the optimal distance and flexibility for this ternary complex formation. The specific binding targets (ligands) used in PhosTAC5 are not disclosed in the search results.
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| ln Vitro |
In vitro, PhosTAC5 has been shown to induce the dephosphorylation of PDCD4 and FOXO3a. PDCD4 is a tumor suppressor that inhibits translation and is regulated by phosphorylation; FOXO3a is a transcription factor involved in apoptosis, cell cycle arrest, and stress resistance, whose activity is modulated by phosphorylation (e.g., by AKT). By inducing dephosphorylation, PhosTAC5 promotes the activation of these tumor suppressors. The specific cellular assays (e.g., Western blotting to detect phosphorylation status, cell viability assays) used to demonstrate these effects are not detailed in the search results. The compound is being explored for its potential in targeting proteins involved in various diseases, including cancer and neurodegenerative disorders.
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| ln Vivo |
In vivo activity data for PhosTAC5 are not available in the provided search results. As a novel chemical biology tool, PhosTAC5 has primarily been characterized in cell-based systems. The compound is being explored for its potential therapeutic applications, including cancer and neurodegenerative disorders, but specific in vivo efficacy, pharmacokinetic, or toxicology data have not been reported. Researchers should consult the primary literature for any updates on in vivo studies.
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| Enzyme Assay |
No specific in vitro enzyme/receptor binding assays are applicable to PhosTAC5, as it is not a traditional inhibitor or ligand. The compound's activity is assessed by evaluating the phosphorylation status of its target proteins. In a typical experiment, cells are treated with PhosTAC5, and the lysates are analyzed by Western blotting using antibodies specific for phosphorylated and total protein. The ratio of phosphorylated to total protein is calculated to determine the degree of dephosphorylation induced by the compound. IC50 values can be calculated from dose-response curves of the phosphorylation signal. A control compound (e.g., a PhosTAC that is inactive) can be used to confirm specificity.
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| Cell Assay |
PhosTAC5 is evaluated in a cell-based assay. Cultured cells (e.g., HEK293, HeLa, or other appropriate cell lines) are seeded in 6-well or 12-well plates and allowed to reach 70-80% confluency. The cells are treated with PhosTAC5 at varying concentrations (e.g., 0.001-10 uM) in complete growth medium for 4-24 h. The compound is typically dissolved in DMSO, and the final DMSO concentration is kept below 0.1%. After the treatment period, the cells are lysed in RIPA buffer containing a phosphatase inhibitor cocktail and a protease inhibitor cocktail. Protein concentrations are measured using the BCA assay. Equal amounts of protein (20-40 ug) are separated by SDS-PAGE and transferred to PVDF membranes. The membranes are probed with primary antibodies against: (1) phospho-PDCD4 (specific site, e.g., S67), (2) total PDCD4, (3) phospho-FOXO3a (specific site, e.g., T32), (4) total FOXO3a, and (5) a loading control such as beta-actin or GAPDH. The membranes are incubated with appropriate HRP-conjugated secondary antibodies, and the signal is detected by enhanced chemiluminescence (ECL). Densitometry is performed using ImageJ to quantify the phosphorylation signal relative to total protein. The percentage of dephosphorylation is calculated as (1 - (phospho/total treated)/(phospho/total control)) × 100%. The EC50 (concentration at which 50% dephosphorylation is achieved) is determined from the dose-response curve. Cell viability should be assessed using an MTT assay to ensure that the observed dephosphorylation is not due to cytotoxicity.
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| Animal Protocol |
No animal protocol is available for PhosTAC5. Since PhosTAC5 is a novel chemical biology tool, it may eventually be tested in animal models of disease, such as tumor xenograft models in mice. Based on its mechanism of reactivating tumor suppressors (PDCD4, FOXO3a) by dephosphorylation, one could hypothesize that PhosTAC5 might be evaluated in cancer models. The compound could be dissolved in a vehicle (e.g., 5% DMSO + 30% PEG300 + 5% Tween 80 + 60% saline) and administered intraperitoneally (i.p.) or intravenously (i.v.) at doses ranging from 1-50 mg/kg, once daily or every other day. Tumor volume and weight would be measured, and the phosphorylation status of PDCD4 and FOXO3a in tumor lysates would be assessed by Western blot. However, no experimental data are available to confirm this protocol.
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| ADME/Pharmacokinetics |
No pharmacokinetic data are available for PhosTAC5. The compound has a molecular weight of 1031.66 g/mol (based on the non-salt form) and contains a PEG-based linker with five PEG units, which might improve solubility and potentially alter PK properties. As a synthetic chimera, it is likely to have a short half-life due to metabolic instability. The compound is supplied as a pure form and should be stored at -20degC for up to 3 years or in solvent at -80degC for up to 6 months. No specific information on bioavailability or clearance is available.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for PhosTAC5. As a novel research tool, comprehensive toxicology studies (e.g., acute, sub-chronic, genotoxicity) have not been reported. Based on its mechanism of reactivating tumor suppressors, there is a theoretical risk of on-target toxicity in normal cells if systemic exposure is achieved. However, no overt toxicity has been reported in the literature. Standard laboratory safety precautions for handling research-grade chemicals should be followed.
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| References |
[1]. Chen PH, et al. Modulation of Phosphoprotein Activity by Phosphorylation Targeting Chimeras (PhosTACs). ACS Chem Biol. 2021 Dec 17;16(12):2808-2815.
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| Additional Infomation |
PhosTAC5 is a research-grade phosphorylation-targeting chimera (PhosTAC) molecule composed of a linker with five PEG groups. It induces the dephosphorylation of PDCD4 and FOXO3a, providing a tool for modulating protein activity post-translationally. PhosTAC5 is not approved for clinical use. This product is for research use only. Store as a pure form at -20degC for 3 years or at 4degC for 2 years, or in solvent at -80degC for 6 months or -20degC for 1 month.
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| Molecular Formula |
C54H79CLN2O15
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| Appearance |
Light yellow to yellow oil
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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) |
DMSO :~100 mg/mL (~96.93 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.) |
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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