Cat. No. 4054
Alternative Name: Ingenol 3-angelate
Chemical Name: (2Z)-2-Methyl-2-butenoic acid (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2
Biological ActivityActivator 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
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.
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.
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.
Kedei et al (2004) Characterization of the interaction of ingenol-3-angelate with protein kinase C. Cancer Res. 64 3243. PMID: 15126366.
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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.
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Keywords: PEP 005, supplier, Ingenol, 3-angelate, PEP005, protein, kinase, C, PKC, activators, anticancer, antileukemic, PKCd, PKCdelta, PKCδ, Tocris Bioscience, Protein Kinase C Activator products
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