Ingenol mebutate gel applied topically for 2 to 3 days is effective for field treatment of actinic keratoses.Ingenol mebutate is a Cell Death Inducer. The physiologic effect of ingenol mebutate is by means of Increased Cellular Death.
|Source||Mol Cancer Ther (2015). Figure 4. Ingenol Mebutate|
|Cell Lines||SCC cells|
|Incubation Time||24 h|
|Results||In addition, we used either the PKC inhibitor AEB071 or a knockdown of PKCd, either alone or in combination with ingenol mebutate and analyzed the expression of ERK target genes. Either inhibition of PKC or knockdown of PKCd could prevent the upregulation of ERK target gene expression after ingenol mebutate treatment|
|Source||Mol Cancer Ther (2015). Figure 3. Ingenol Mebutate|
|Cell Lines||SCC13 cells|
|Incubation Time||24 h|
|Results||Similar to our findings with the PKC inhibitor, we detected a rescue of cell viability upon ingenol mebutate treatment when PKCd was knocked down. A knockdown PKCa followed by ingenol mebutate treatment led only to a partial rescue, while PKCd knockdown could rescue the ingenol mebutate–treated cells completely|
|Cell lines||T7 cell|
|Preparation method||Tumours were treated topically (on days 4 and 5 post tumour inoculation) with 30 μl of 0.25 % (w/v) ingenol mebutate or placebo gel (supplied by LEO Pharma A/S) using a positive displacement pipette, with the gel then spread over the tumour site.|
|Concentrations||30 μl of 0.25 % (w/v)|
|Incubation time||48 h|
|Animal models||BALB/c nu−/nu− mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||41 mg/ml in CHCl3|
Effective treatment of squamous cell carcinomas with ingenol mebutate gel in immunologically intact SKH1 mice.
Cozzi SJ, et al. Arch Dermatol Res. 2013 Jan;305(1):79-83. PMID: 22871992.
Ingenol mebutate gel for actinic keratosis.
Lebwohl M,et.al. N Engl J Med. 2012 Mar 15;1010-9. PMID: 22417254.
|Related PKC Products|
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
|Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
Ro 31-8220 is a protein kinase C inhibitor, with activity at other protein kinases (IC50 values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.