PEP 005

Biological Activity

PEP 005 is an 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 reactivates hypofunctional CD8⁺ T cells during chronic viral infection. Acts as a substrate for multidrug transporter.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC.
   Hampson et al.
   Blood, 2005;106:1362
2. Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells.
   Benhadji et al.
   Br.J.Cancer, 2008;99:1808
3. The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature.
   Li et al.
   Cancer Res., 2010;70:4509
4. Characterization of the interaction of ingenol-3-angelate with protein kinase C.
   Kedei et al.
   Cancer Res., 2004;64:3243
5. Synergistic reactivation of latent HIV expression by Ingenol-3-Angelate, PEP005, targeted NF-kB signaling in combination with JQ1 induced p-TEFb activation.
   Jiang et al.
   PLoS Pathog., 2015;11:e1005066
6. Discovery of small molecules for the reversal of T cell exhaustion.
   Marro et al.
   Cell Rep., 2019;29:3293

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