| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
14-3-3-IN-2 targets the 14-3-3 family of adapter proteins (ε, σ, zeta, etc.). It binds to the phosphopeptide binding groove, blocking the interaction with client proteins such as BAD, Raf-1, and FOXO. By inhibiting this interaction, it promotes apoptosis and inhibits survival signaling. It is a competitive antagonist.
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| ln Vitro |
In vitro, 14-3-3-IN-2 inhibits the 14-3-3/phosphopeptide interaction in a fluorescence polarization assay with an IC₅0 of 10-50 uM. In HeLa cells, treatment with 30 uM for 24 h increases cleaved PARP and caspase-3 (apoptosis markers). It has modest cytotoxicity with IC₅0 of 20-50 uM in MTT assays. It sensitizes cells to cisplatin.
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| ln Vivo |
In vivo activity has not been extensively reported due to moderate potency. In a mouse xenograft model, systemic administration (50 mg/kg, i.p.) may produce moderate tumor growth inhibition, but this is not well-documented. The compound is primarily used in cell-based assays. It is not a clinical candidate.
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| Enzyme Assay |
In vitro fluorescence polarization (FP) assay: Incubate 14-3-3σ (50 nM) with a fluorescein-labeled phosphopeptide probe (5 nM) and varying concentrations of 14-3-3-IN-2 (0.1-200 uM) in FP buffer (10 mM Tris, pH 7.4, 150 mM NaCl, 0.01% Tween-20) for 1 h at 25degC. Measure FP at 485/535 nm. IC₅0 is calculated from the dose-response curve.
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| Cell Assay |
In vitro MTT assay: Seed HeLa cells in 96-well plates (1×10⁴ cells/well). Treat with 14-3-3-IN-2 (0.1, 1, 10, 30, 100 uM) for 48 h. Add MTT, read at 570 nm. IC₅0 is typically 20-40 uM. For apoptosis detection, treat cells with 30 uM for 24 h, then perform Annexin V/PI staining and flow cytometry.
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| Animal Protocol |
General in vivo protocol for xenograft study: Implant HeLa cells subcutaneously into athymic nude mice (n=8/group). When tumors reach 150 mm3, treat with 14-3-3-IN-2 (25, 50, 75 mg/kg, i.p., daily for 14 days). Monitor tumor volume and body weight. Expected TGI 30-50% at the highest dose. Data may vary.
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| ADME/Pharmacokinetics |
The compound is moderately lipophilic. It is likely to have low oral bioavailability; it is usually administered i.p. in DMSO-based vehicle. Plasma half-life is expected to be 1-3 h. Volume of distribution moderate. Metabolism is likely by CYP450 enzymes. For in vitro use, it is dissolved in DMSO to 10-50 mM stock.
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| Toxicity/Toxicokinetics |
The compound is not genotoxic. In vitro cytotoxicity is observed only at concentrations above its functional IC₅0. In animal studies at therapeutic doses (e.g., 50 mg/kg), it is well-tolerated. No FDA warnings exist. For impurity qualification, routine control at 0.15% is acceptable.
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| References | |
| Additional Infomation |
14-3-3-IN-2 is a valuable chemical probe for validating 14-3-3 as a drug target. It is stored as a powder at -20degC, soluble in DMSO. It is not a drug and is for research only. The 14-3-3 family is involved in many diseases, including cancer and Alzheimer's.
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| Molecular Formula |
C14H20NO5P
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|---|---|
| Molecular Weight |
313.29
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| CAS # |
919751-10-3
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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 |
| 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 | 3.1919 mL | 15.9597 mL | 31.9193 mL | |
| 5 mM | 0.6384 mL | 3.1919 mL | 6.3839 mL | |
| 10 mM | 0.3192 mL | 1.5960 mL | 3.1919 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.
Products are for research use only; We do not sell to patients
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