PEP 005

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Cat.No. 4054 - PEP 005 | C25H34O6 | CAS No. 75567-37-2
Description: Protein kinase C activator
Alternative Names: Ingenol 3-angelate
Chemical Name: (2Z)-2-Methyl-2-butenoic acid (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2,5,5a,6,9,10,10a-octahydro-5,5a-dihydroxy-4-(hydroxymethyl)-1,1,7,9-tetramethyl-11-oxo-1H-2,8a-methanocyclopenta[a]cyclopropa[e]cyclodecen-6-yl ester
Purity: ≥98% (HPLC)
Citations (1)

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
Smiles CC([C@@H]2OC(/C(C)=C\C)=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
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.

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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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet


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

If you know of a relevant reference for PEP 005, please let us know.

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1 Citation for PEP 005

Citations are publications that use Tocris products. Selected citations for PEP 005 include:

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

Do you know of a great paper that uses PEP 005 from Tocris? If so please let us know.

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Pathways for PEP 005


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