PEP 005
Tocris Bioscience, part of Bio-Techne | Catalog # 4054
Protein kinase C activator
Discontinued Product
4054 has been discontinued.
View all Protein Kinase C Activators products.
Key Product Details
Description
Protein kinase C activator
Alternative Names
Ingenol 3-angelate,Ingenol Mebutate
Product Description
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.Product Specifications
Molecular Weight
430.53
Formula
C25H34O6
Storage
Store at -20°C
Purity
≥97% (HPLC)
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
CAS Number
75567-37-2
PubChem ID
6918670
InChI Key
VDJHFHXMUKFKET-WDUFCVPESA-N
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 0.86 | 2 |
Preparing Stock Solutions
for PEP 005
The following data is based on the product molecular weight 430.53
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.02 mM | 116.14 mL | 580.68 mL | 1,161.36 mL |
| 0.1 mM | 23.23 mL | 116.14 mL | 232.27 mL |
| 0.2 mM | 11.61 mL | 58.07 mL | 116.14 mL |
| 1 mM | 2.32 mL | 11.61 mL | 23.23 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Marro Discovery of small molecules for the reversal of T cell exhaustion. Cell Rep. 2019 PMID: 31801090
- Jiang 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. 2015 PMID: 26225771
- Hampson PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood 2005 PMID: 15845901
- Kedei Characterization of the interaction of ingenol-3-angelate with protein kinase C. Cancer Res. 2004 PMID: 15126366
- Li The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature. Cancer Res. 2010 PMID: 20460505
- Benhadji 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 2008 PMID: 19034280
Product Specific Notices for PEP 005
For research use only
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