Biological Activity
Activator of protein kinase C (PKC). Exhibits antileukemic activity; induces nuclear translocation of PKCδ, and induces apoptosis in acute myeloid leukemia (AML) cell lines and primary AML blast cells. Also displays antiproliferative effects and induces apoptosis in Colo205 cells. Reactivates latent HIV in cell culture. Also acts as a substrate for multidrug transporter.
Technical Data
| M. Wt | 430.53 |
| Formula | C25H34O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 75567-37-2 |
| PubChem ID | 6918670 |
| InChI Key | VDJHFHXMUKFKET-WDUFCVPESA-N |
| Smiles | CC([C@@H]2OC(/C(C)=CC)=O)=C[C@@]1([C@H](C)C4)[C@]2(O)[C@H](O)C(CO)=C[C@]([C@@]3([H])[C@]4([H])C(C)3C)([H])C1=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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 0.86 | 2 |
Preparing Stock Solutions
The following data is based on the product molecular weight 430.53. 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 | 2.32 mL | 11.61 mL | 23.23 mL |
| 5 mM | 0.46 mL | 2.32 mL | 4.65 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.32 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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References
References are publications that support the products' biological activity.
Benhadji et al (2008) Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells. Br.J.Cancer 99 1808 PMID: 19034280
Li et al (2010) The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature. Cancer Res. 70 4509 PMID: 20460505
Kedei et al (2004) Characterization of the interaction of ingenol-3-angelate with protein kinase C. Cancer Res. 64 3243 PMID: 15126366
Hampson et al (2005) PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood 106 1362 PMID: 15845901
Jiang et al (2015) Synergistic reactivation of latent HIV expression by Ingenol-3-Angelate, PEP005, targeted NF-kB signaling in combination with JQ1 induced p-TEFb activation. PLoS Pathog. 11 e1005066 PMID: 26225771
Keywords: PEP 005, supplier, Ingenol, 3-angelate, PEP005, protein, kinase, C, PKC, activators, anticancer, antileukemic, PKCd, PKCdelta, PKCδ, Ingenol, 3-angelate, Protein, Kinase, C, Multidrug, Transporters, Protein, Kinase, C, Tocris Bioscience
