Biological Activity
Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells in vitro and in vivo. Displays no effect on the growth of normal prostate epithelial RPWE-1 cells at concentrations of 10 and 20 μM.
Technical Data
| M. Wt | 2820.33 |
| Formula | C111H211N59O26S |
| Sequence | GGGRRRRRRRRGCKKPGLRRRQT |
| Storage | Store at -20°C |
| PubChem ID | 90488955 |
| InChI Key | AIRNEKGCZRAELC-NBQUZRIMSA-N |
| Smiles | [H]NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)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 2 mg/ml in 20% acetonitrile / water |
Preparing Stock Solutions
The following data is based on the product molecular weight 2820.33. 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 | 0.35 mL | 1.77 mL | 3.55 mL |
| 5 mM | 0.07 mL | 0.35 mL | 0.71 mL |
| 10 mM | 0.04 mL | 0.18 mL | 0.35 mL |
| 50 mM | 0.01 mL | 0.04 mL | 0.07 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Morishita et al (2011) Cell-permeable carboxyl-terminal p27Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase. J.Biol.Chem. 286 2681 PMID: 21062737
Keywords: R8-T198wt, supplier, anticancer, prostate, cancer, Pim-1, kinases, inhibits, inhibitors, DU145, cells, cell, lines, p27Kip1, Pim, Kinase, Pim, Kinase, Tocris Bioscience
