| Size | Price | Stock | Qty |
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| 10mg |
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| ln Vitro |
The active component of Euphorbia peplus, ingenol mebutate (also known as ingenol 3-angelate), is a strong PKC activator, with Kis values of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, in that order. The EC50 of ingenium xylenol methyl butyl ester is 13 ± 2.4 nM (PKC-α), 4.37 ± 0.4 nM (PKC-βI), 10.5 ± 2.2 nM (PKC-βII), 38.6 ± 2.9 nM (PKC-δ) , 1.08 ± 0.01 nM (PKC-ε), 0.9 ± 0.13 nM (PKC-μ), 198 ± 12.5 nM (PKC-α), 69.1 ± 8.2 nM (PKC-βI), 4.6 ± 0.4 nM in WEHI-231 cells (PKC-ε) and 1 nM (PKC-μ), 635 ± 245 nM (PKC-α), 146 ± 35 nM (PKC-βI), 4.7 ± 0.7 nM (PKC-δ), 1.1 in HOP-92 cells ± 0.5 nM (PKC-ε) and 30 nM (PKC-μ) in Colo-205 cells. WEHI-231 cells, HOP-92, and Colo-205 cells are sensitized by ingenol mebutate, with IC50 values of 1.41 ± 0.255 nM, 3.24 ± 2.01 nM, and 11.9 ± 1.307 nM, in that order [1]. PKC-δ-dependent, ingenol mebutate (PEP005; 20 nM) can cause apoptosis in primary AML bone marrow blasts but not in normal myeloblasts [2]. PKCδ is inhibited while PKCα is activated by ingenol mebutate (PEP005). Compared to the parent Colo205-S cells, Colo205-R cells have an IC50 of >10 μM, which makes them more than 300 times more resistant to ingenol methyl butyl ester [3].
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| References |
[1]. 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.
[2]. 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. [3]. 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 |
| Molecular Formula |
C25H34O6
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|---|---|
| Molecular Weight |
430.53
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| Exact Mass |
430.23554
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| CAS # |
75567-37-2
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| Related CAS # |
Ingenol;30220-46-3
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| SMILES |
C\C=C(C)/C(=O)O[C@@H]1[C@]2(O)[C@]3(C=C1C)C(=O)[C@@H](C=C(CO)[C@H]2O)[C@@H]4C(C)(C)[C@@H]4C[C@H]3C
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| Synonyms |
PEP 005; PEP-005; PEP005
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~232.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3227 mL | 11.6136 mL | 23.2272 mL | |
| 5 mM | 0.4645 mL | 2.3227 mL | 4.6454 mL | |
| 10 mM | 0.2323 mL | 1.1614 mL | 2.3227 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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