Ingenol Mebutate (Synonyms: 巨大戟醇甲基丁烯酸酯; Ingenol 3-angelate; PEP005)

目录号: HY-B0719 纯度: 99.65%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Ingenol Mebutate 是 Euphorbia peplus 中的活性成分，为 PKC 的调节剂，对 PKC-α，PKC-β，PKC-γ，PKC-δ 和 PKC-ε 的 K_i 值分别为 0.3，0.105，0.162，0.376 和 0.171 nM。

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Ingenol Mebutate Chemical Structure

CAS No. : 75567-37-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2586	In-stock
1 mg	￥868	In-stock
5 mg	￥2730	In-stock
10 mg	￥4508	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

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Ingenol Mebutate (Standard) 询价

MCE 顾客使用本产品发表的 3 篇科研文献

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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)

细胞效力
(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]

体外研究
(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].

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

Clinical Trial

分子量

430.53

Formula

C₂₅H₃₄O₆

CAS 号

75567-37-2

性状

固体

颜色

White to off-white

中文名称

巨大戟醇甲基丁烯酸酯

结构分类

初始来源

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (232.27 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.81 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.81 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.81 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.65%

选择批次：

Data Sheet (635 KB) SDS (394 KB)

COA (298 KB) HNMR (257 KB) LCMS (89 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Cell Assay ^[2]	KG1a cells are transiently transfected with EGFP-tagged mouse PKC-δ subcloned into pEGFP-N1 plasmid using an Amaxa nucleofection apparatus. Cells are treated with Ingenol Mebutate (0.2 μM-20 μM) 24 hours after transfection. Cell viability in EGFP-positive cells is assessed and loss of viability confirmed in the total cell culture by MTT assay after 3 days. Briefly, 24 hours after transfection, 2 × 10⁴ cells are plated in 5 wells in 96-well plates and exposed to 0, 0.2, 2, and 20 μM Ingenol Mebutate. At 72 hours, 20 μL MTT substrate at 5 mg/mL is added and plates are incubated at 37°C. After 3 hours, 150 μL media is removed and replaced with 200 μL dimethyl sulfoxide (DMSO). Absorbance at an optical density (OD) of 550 nm is read on a plate reader and corrected for absorbance obtained from blank media controls^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Cell Assay
^[2]

KG1a cells are transiently transfected with EGFP-tagged mouse PKC-δ subcloned into pEGFP-N1 plasmid using an Amaxa nucleofection apparatus. Cells are treated with Ingenol Mebutate (0.2 μM-20 μM) 24 hours after transfection. Cell viability in EGFP-positive cells is assessed and loss of viability confirmed in the total cell culture by MTT assay after 3 days. Briefly, 24 hours after transfection, 2 × 10⁴ cells are plated in 5 wells in 96-well plates and exposed to 0, 0.2, 2, and 20 μM Ingenol Mebutate. At 72 hours, 20 μL MTT substrate at 5 mg/mL is added and plates are incubated at 37°C. After 3 hours, 150 μL media is removed and replaced with 200 μL dimethyl sulfoxide (DMSO). Absorbance at an optical density (OD) of 550 nm is read on a plate reader and corrected for absorbance obtained from blank media controls^[2].

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

参考文献

[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]

Ingenol Mebutate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3227 mL	11.6136 mL	23.2272 mL	58.0680 mL
	5 mM	0.4645 mL	2.3227 mL	4.6454 mL	11.6136 mL
	10 mM	0.2323 mL	1.1614 mL	2.3227 mL	5.8068 mL
	15 mM	0.1548 mL	0.7742 mL	1.5485 mL	3.8712 mL
	20 mM	0.1161 mL	0.5807 mL	1.1614 mL	2.9034 mL
	25 mM	0.0929 mL	0.4645 mL	0.9291 mL	2.3227 mL
	30 mM	0.0774 mL	0.3871 mL	0.7742 mL	1.9356 mL
	40 mM	0.0581 mL	0.2903 mL	0.5807 mL	1.4517 mL
	50 mM	0.0465 mL	0.2323 mL	0.4645 mL	1.1614 mL
	60 mM	0.0387 mL	0.1936 mL	0.3871 mL	0.9678 mL
	80 mM	0.0290 mL	0.1452 mL	0.2903 mL	0.7258 mL
	100 mM	0.0232 mL	0.1161 mL	0.2323 mL	0.5807 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ingenol Mebutate75567-37-2Ingenol 3-angelate PEP005巨大戟醇甲基丁烯酸酯PEP005PEP 005PEP-005PKCProtein kinase CInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Ingenol Mebutate (Synonyms: 巨大戟醇甲基丁烯酸酯; Ingenol 3-angelate; PEP005)

Customer Review

Other Forms of Ingenol Mebutate:

MCE 顾客使用本产品发表的 3 篇科研文献