PEP 005

Cat. No. 4054

PEP 005 C25H34O6 [75567-37-2]

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Alternative Name: 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

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
Solubility:
Soluble to 2 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
75567-37-2

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

References are publications that support the products' biological activity.

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.

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

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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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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