Biological Activity
Selective cell-permeable peptide inhibitor of protein kinase C (IC50 ~ 0.5 μM). Consists of amino acids 19 - 31 of PKC pseudosubstrate domain linked by a disulphide bridge to a cell permeabilisation Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the inhibitor peptide.
Technical Data
| M. Wt | 3994.84 |
| Formula | C177H294N62O38S3 |
| Sequence |
CRQIKIWFQNRRMKWKK CRFARKGALRQKNV* (Modifications: Disulfide bridge between 17 -1*) |
| Storage | Store at -20°C |
| CAS Number | 172308-76-8 |
| PubChem ID | 90488712 |
| InChI Key | KIWJPYSSLFMLBZ-OSCDWKIESA-N |
| Smiles | [H]N[C@@H](CSSC[C@H](N[H])C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3994.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 5 mM | 0.05 mL | 0.25 mL | 0.5 mL |
| 10 mM | 0.03 mL | 0.13 mL | 0.25 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.05 mL |
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Product Datasheets
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References
References are publications that support the products' biological activity.
Derossi et al (1994) The third helix of the antennapedia homeodomain translocates through biological membranes. J.Biol.Chem. 269 10444 PMID: 8144628
House and Kemp (1987) Protein kinase C contains a pseudosubstrate prototope in its regulatory domain. Science 238 1726 PMID: 3686012
Theodore et al (1995) Intraneuronal delivery of protein kinase C pseudosubstrate leads to growth cone collapse. J.Neurosci. 15 7158 PMID: 7472470
Keywords: PKC b pseudosubstrate, supplier, Selective, cell-permeable, PKC, inhibitors, inhibits, Protein, Kinases, C, beta, pseudosubstrate, PKCb, Protein, kinase, C, beta, pseudosubstrate, Protein, Kinase, C, Protein, Kinase, C, Tocris Bioscience
