| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Peptidyl-prolyl cis-trans isomerase Pin1 (PPIase) is the primary molecular target. This enzyme catalyzes the isomerization of the peptide bond preceding a proline residue, which regulates the conformation and function of phosphorylated proteins involved in cell cycle progression and oncogenesis. The substrate is cleaved by Pin1 at the Pro-Phe bond.
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| ln Vitro |
In cell-free assays, Suc-Ala-Glu-Pro-Phe-pNA is a highly specific chromogenic substrate for Pin1. Upon enzymatic cleavage, pNA is released, producing a bright yellow color measurable at 390-405 nm. The Michaelis constant (Km) for Pin1 is in the low micromolar range. This substrate can be used to evaluate the inhibitory effect of candidate compounds on Pin1 and to determine the catalytic activity of purified Pin1 enzyme.
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| Enzyme Assay |
A typical enzyme kinetic assay: Pin1 (0.1-1 uM) is incubated with varying concentrations of Suc-Ala-Glu-Pro-Phe-pNA (0-500 uM) in an assay buffer (35 mM HEPES, pH 7.8, 75 mM NaCl, 0.05% Tween-20, and 5 mM DTT) at 25degC. The increase in absorbance at 390 nm (ε = 12,000 M-¹cm-¹) is monitored continuously for 5-10 minutes. Initial reaction rates are plotted against substrate concentration to determine kinetic parameters.
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| Cell Assay |
For cellular experiments, cells are lysed and the lysate is incubated with Suc-Ala-Glu-Pro-Phe-pNA (100-400 uM) in the assay buffer for 60-120 minutes at 37degC. The absorbance at 390 nm is measured to determine cellular Pin1 activity. Specific Pin1 inhibitors (e.g., juglone or PiB) can be used to confirm that the measured activity is due to Pin1.
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| Animal Protocol |
There is no standard in vivo protocol for this substrate, as it is a cell-impermeable chromogenic reagent designed for in vitro use. For in vivo Pin1 activity studies, alternative approaches such as fluorescent probes or bioluminescent substrates are used. Suc-AEPF-pNA is strictly a biochemical assay tool.
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| ADME/Pharmacokinetics |
PK properties are not applicable as this substrate is not administered in vivo. It is formulated as a stock solution (10-50 mM) in DMSO or in assay buffer (with 5-10% DMSO) for enzymatic assays. Stock solutions should be stored at -20degC and protected from light to prevent degradation.
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| Toxicity/Toxicokinetics |
Toxicity of Suc-Ala-Glu-Pro-Phe-pNA is low at typical assay concentrations (10-500 uM). The released pNA product is moderately toxic if ingested, but at laboratory scale, standard safety precautions (gloves, lab coat) are sufficient. Avoid skin contact and inhalation of powder. The compound is for research use only.
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| References |
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| Additional Infomation |
Suc-Ala-Glu-Pro-Phe-pNA is a standard chromogenic substrate for Pin1, a key regulator of the cell cycle and a promising therapeutic target for cancer, Alzheimer's disease, and asthma. The proline residue in the sequence is critical for Pin1 recognition. This substrate is used in high-throughput screening campaigns to discover novel Pin1 inhibitors for drug development.
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| Molecular Formula |
C32H38N6O11
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|---|---|
| Molecular Weight |
682.68
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| Exact Mass |
682.259
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| CAS # |
128802-76-6
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| Related CAS # |
Suc-Ala-Glu-Pro-Phe-pNA TFA
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| PubChem CID |
91886559
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1165.4±65.0 °C at 760 mmHg
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| Flash Point |
658.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
2.19
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
49
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| Complexity |
1230
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)NC3=CC=C(C=C3)[N+](=O)[O-])NC(=O)CCC(=O)O
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| InChi Key |
NXIHRDNJQWUSLK-KMAVCZJNSA-N
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| InChi Code |
InChI=1S/C32H38N6O11/c1-19(33-26(39)14-16-28(42)43)29(44)35-23(13-15-27(40)41)32(47)37-17-5-8-25(37)31(46)36-24(18-20-6-3-2-4-7-20)30(45)34-21-9-11-22(12-10-21)38(48)49/h2-4,6-7,9-12,19,23-25H,5,8,13-18H2,1H3,(H,33,39)(H,34,45)(H,35,44)(H,36,46)(H,40,41)(H,42,43)/t19-,23-,24-,25-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-(3-carboxypropanoylamino)propanoyl]amino]-5-[(2S)-2-[[(2S)-1-(4-nitroanilino)-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-oxopentanoic acid
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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) |
DMSO: 125 mg/mL (183.10 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 | 1.4648 mL | 7.3241 mL | 14.6482 mL | |
| 5 mM | 0.2930 mL | 1.4648 mL | 2.9296 mL | |
| 10 mM | 0.1465 mL | 0.7324 mL | 1.4648 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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