Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Ingenol Mebutate [75567-37-2]

Stampa

Cat# HY-B0719-1mg

Size : 1mg

Contatta il distributore locale :

Telefono : +1 850 650 7790

Marca : MedChemExpress

Richiedere ulteriori informazioni

Contatta il distributore locale :

Telefono : +1 850 650 7790

Description

Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with K_is 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, respectively, and has antiinflammatory and antitumor activity.

IC₅₀ & Target^[1]

PKC-β

0.105 nM (Ki)

PKC-γ

0.162 nM (Ki)

PKC-ε

0.171 nM (Ki)

PKC-α

0.3 nM (Ki)

PKC-δ

0.376 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
Keratinocyte	EC₅₀	10.3 nM Compound: 1, PEP005, Ingenol mebutate	Induction of IL-8 release in human primary epidermal keratinocytes after 6 hrs by HTRF assay Induction of IL-8 release in human primary epidermal keratinocytes after 6 hrs by HTRF assay	[PMID: 23993332]
Keratinocyte	EC₅₀	10.3 nM Compound: 1, PEP005, Picato, ingenol mebutate	Induction of proimflammatory activity in human primary epidermal keratinocytes assessed as IL-8 release after 6 hrs Induction of proimflammatory activity in human primary epidermal keratinocytes assessed as IL-8 release after 6 hrs	[PMID: 24332494]
Keratinocyte	EC₅₀	11.2 nM Compound: 1, PEP005, Picato, ingenol mebutate	Induction of proimflammatory activity in human primary epidermal keratinocytes assessed as TNFalpha release after 6 hrs Induction of proimflammatory activity in human primary epidermal keratinocytes assessed as TNFalpha release after 6 hrs	[PMID: 24332494]
Keratinocyte	EC₅₀	11.2 nM Compound: 1, PEP005, Ingenol mebutate	Induction of TNFalpha release in human primary epidermal keratinocytes after 6 hrs Induction of TNFalpha release in human primary epidermal keratinocytes after 6 hrs	[PMID: 23993332]
MT4	CC₅₀	> 9.3 μM Compound: 22	Cytotoxicity against human MT4 cells after 3 days by CytoTox-Glo assay Cytotoxicity against human MT4 cells after 3 days by CytoTox-Glo assay	[PMID: 30031972]
MT4	EC₅₀	17 nM Compound: 27	Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
MT4	EC₅₀	9 nM Compound: 27	Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
U-937	CC₅₀	> 200 nM Compound: Ingenol 3A	Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 29541372]
Vero	EC₅₀	22.9 μM Compound: 27	Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days	[PMID: 25970561]

In Vitro

Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus, acting as a potent PKC activator, with K_is 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, respectively. Ingenol Mebutate also EC₅₀s of 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) in WEHI-231 cells, 198 ± 12.5 nM (PKC-α), 69.1 ± 8.2 nM (PKC-βI), 4.6 ± 0.4 nM (PKC-ε) and 1 nM (PKC-μ) in HOP-92 cells, 635 ± 245 nM (PKC-α), 146 ± 35 nM (PKC-βI), 4.7 ± 0.7 nM (PKC-δ), 1.1 ± 0.5 nM (PKC-ε), and 30 nM (PKC-μ) in Colo-205 cells. Ingenol Mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells, with IC₅₀s of 1.41 ± 0.255 nM, 3.24 ± 2.01 nM, and 11.9 ± 1.307 nM, respectively^[1]. Ingenol Mebutate (PEP005; 20 nM) actions are PKC-δ dependent, induces apoptosis in primary AML marrow blasts but not in normal myeloblasts^[2]. Ingenol Mebutate (PEP005) activates PKCδ and inhibits PKCα. Colo205-R cells (IC₅₀: >10 μM) are >300-fold more resistant to Ingenol Mebutate than parental Colo205-S cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (232.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.65%

Fiche technique (287 KB) SDS (394 KB)

COA (260 KB) HNMR (291 KB) LCMS (89 KB)

Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Si può anche essere interessati nei seguenti prodotti:

Cat#

Descrizione

Cond.

Priced

HY-B0719-5mg

Ingenol Mebutate [75567-37-2]

5mg

KN420731

E Cadherin (CDH1) Human Gene Knockout Kit (CRISPR)

1kit

Ingenol Mebutate [75567-37-2]

Cat# HY-B0719-1mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Ingenol Mebutate Related Antibodies

Si può anche essere interessati nei seguenti prodotti: