Ingenol mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
Ingenol Mebutate/巨大戟醇甲基丁烯酸酯 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse striatal/accumbal slices
1 μM
90 min
To examine the effect of PKC activator on β-PIX phosphorylation
Mol Psychiatry. 2022 Aug;27(8):3479-3492.
HuT-78 cells
50 nM
24 h
Investigate PEP005-mediated loss of MMP and ROS production
Cells. 2025 Apr 3;14(7):535
HH and HuT-78 cells
50 nM
24 h
Study PEP005-induced apoptosis and cell viability restoration
Cells. 2025 Apr 3;14(7):535
CTCL cell lines
50 nM
24 h
Investigate the effects of PEP005 on PKCδ proform
Cells. 2025 Apr 3;14(7):535
B16 melanoma cells
40 ng/ml
1 day
To study the killing effect of ingenol mebutate on B16 cells. Results showed that ingenol mebutate significantly promoted the killing of B16 cells.
PLoS One. 2016 Apr 21;11(4):e0153975
Human adult epidermal keratinocytes (HEKa-APF)
50 μg/ml
16 hours
To investigate whether ingenol mebutate induces IL-1α release from keratinocytes. Results showed that 50 μg/ml ingenol mebutate treatment caused the release of 18 kDa IL-1α.
PLoS One. 2016 Apr 21;11(4):e0153975
HBL-6, JSC-1, BC2 and BC3 cells
≤100 nM
PEP005 also triggered KSHV lytic replication in these cell lines, and lower concentrations (≤100 nM) did not significantly induce cell death.
Mol Cancer Ther. 2017 Nov;16(11):2627-2638
TREx K-Rta BCBL-1 cells
10–1,000 nM
48 hours
PEP005 triggers KSHV lytic replication in a dose-dependent manner, at a concentration as low as 10 nM. High concentrations of PEP005 (500–1,000 nM) demonstrated apparent cell toxicity at 48 hours post-treatment.
Mol Cancer Ther. 2017 Nov;16(11):2627-2638
Mesenchymal stem cells (MSCs)
0.1-3 µg/mL
24 hours
Enhance the B cell inhibitory potential of MSCs, inhibiting IgM production by B cells through TGF-β1 and IL-1β-dependent mechanisms.
Int J Mol Sci. 2024 Nov 25;25(23):12625
CD3+CD8+ T cells
250 nM
5 days
IngMb treatment significantly increased the number of YFP-expressing CD3+CD8+ T cells, indicating its ability to enhance T cell proliferation and effector functions.
Cell Rep. 2019 Dec 3;29(10):3293-3302. e3
LCMV-GP 33-41-specific CD8+ T cells
250 nM
5 days
IngMb treatment significantly increased YFP expression and IFN-γ production, indicating its ability to restore the function of exhausted T cells.
Cell Rep. 2019 Dec 3;29(10):3293-3302. e3
Primary human epidermal keratinocytes
100 nM
72 hours
Evaluate the effect of Ingenol Mebutate and Ingenol Disoxate on cell proliferation. Results showed that Ingenol Disoxate significantly inhibited cell proliferation and induced the expression of keratinocyte differentiation markers.
To investigate the anti-tumor efficacy of ingenol mebutate and its mechanism. Results showed that relapse rates were significantly increased in MyD88-/- mice and anakinra-treated C57BL/6 mice, indicating that IL-1 plays a significant role in the anti-cancer efficacy of ingenol mebutate by promoting neutrophil anti-tumor activity.
PLoS One. 2016 Apr 21;11(4):e0153975
NOD/SCID mice
PEL xenograft tumor model
Intraperitoneal injection
10 µg/kg
Daily for 10 days
JQ1 alone completely inhibited tumor growth, extending median survival from 12 to 23 days. Combination of JQ1 with PEP005 further delayed tumor development, extending median survival to 30.5 days.
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