| Description | Ingenol mebutate (Ingenol 3-Angelate) is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity. |
| In vitro | Ingenol mebutate shows EC50s for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-δ, PKC-ε and PKC-μ of 13, 4.37, 10.5, 38.6, 1.08 and 0.9 nM in WEHI-231 cells. The EC50s are 198, 69.1, 4.6, 1 nM in HOP-92 cells for PKC-α, PKC-βI, PKC-ε, PKC-μ and 635, 146, 4.7, 1.1, 30 nM for PKC-α, PKC-βI, PKC-δ, PKC-ε, PKC-μ in Colo-205 cells. Ingenol mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells with IC50s of 1.41, 3.24, and 11.9 nM, respectively[2]. Ingenol mebutate (20 nM) induces apoptosis in a PKC-δ dependent manner in primary AML marrow blasts but not in normal myeloblasts[3]. |
| Target activity | PKCδ:0.376 nM (Ki), PKCα:0.3 nM (Ki), PKCγ:0.162 nM (Ki), PKCε:0.171 nM (Ki), PKCβ:0.105 nM (Ki) |
| Synonyms | Ingenol 3-Angelate, 巨大戟醇甲基丁烯酸酯, PEP005 |
| molecular weight | 430.53 |
| Molecular formula | C25H34O6 |
| CAS | 75567-37-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90 mg/mL (209 mM) |
| References | 1. Ghoul A, et al. Epithelial-to-mesenchymal transition and resistance to ingenol 3-angelate, a novel protein kinase C modulator, in colon cancer cells. Cancer Res. 2009 May 15;69(10):4260-9. 2. Kedei N, et al. Characterization of the interaction of ingenol 3-angelate with protein kinase C. Cancer Res. 2004 May 1;64(9):3243-55. 3. Hampson P, et al. PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood. 2005 Aug 15;106(4):1362-8. |