U0126

目录号: HY-12031A 纯度: 98.45%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

U0126 是一种有效，非 ATP 竞争性的，选择性的 MEK1 和 MEK2 抑制剂，IC₅₀ 分别为 72 nM 和 58 nM。U0126 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 抑制剂。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

U0126 Chemical Structure

CAS No. : 109511-58-2

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1320	In-stock
5 mg	￥1200	In-stock
10 mg	￥1920	In-stock
25 mg	￥3650	In-stock
50 mg	￥5500	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of U0126:

U0126-EtOH In-stock

MCE 顾客使用本产品发表的 360 篇科研文献

RT-PCR

IHC

: U0126 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2023 Mar 7;115489. [Abstract]; U0126 (20 uM; pretreat for 2 h) rescues the loss of UHRF1/DNMT1 expression and the increase of E-Cadherin expression that induced by Lenvatinib in Huh7 cells.

: U0126 purchased from MCE. Usage Cited in: Mol Cell Endocrinol. 2023 Feb 17;111891. [Abstract]; U0126 (10 uM; pre-treate for 1 h) attenuates IL-1-induced upregulation of COX-2 expression in KGN cells.

: U0126 purchased from MCE. Usage Cited in: Cancer Res. 2019 Sep 1;79(17):4466-4479. [Abstract]; Western blot and IHC analyses for p-ERK1/2 in lung tissues after vehicle or U0126 treatment.

: U0126 purchased from MCE. Usage Cited in: Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F660-F673. [Abstract]; Western analysis of α-SMA, Collagen I and E-cadherin protein expression in the treatment of U0126 with different concentrations.

: U0126 purchased from MCE. Usage Cited in: Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F660-F673. [Abstract]; Western analysis of Vimentin, E-cadherin and Snail1 protein expression with or without the treatment of U0126.

: U0126 purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331. [Abstract]; U0126 enhances the negative effect of Fsk-IBMX on the development of glioma stem cells (GSCs).

: U0126 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2019 Apr 1;51(4):365-374. [Abstract]; MAPKs inhibitors suppress LPS-induced COX-2 expression and AKT1 phosphorylation. RAW264.7 cells are pretreated for 1 h with U0126, SB202190, SP600125 alone, or all the three inhibitors, respectively, and then exposed to 40 ng/ml LPS for 30 min or 12 h. The phosphorylated protein kinases and COX-2 expression are detected by western blot analysis using their corresponding antibodies.

: U0126 purchased from MCE. Usage Cited in: Blood. 2018 Jul 12;132(2):210-222. [Abstract]; Phosphorylation of p-ERK1/2 and p-Akt in MKs pretreated with 0.5 μM NVP-ADW742, 10 μM U0126 or 20 μM LY294002 followed by rhIGF-1 treatment for 15 minutes.

: U0126 purchased from MCE. Usage Cited in: Biomaterials. 2018 Sep;178:95-108. [Abstract]; U0126 effectively inhibits the phosphorylation of ERK, leading to the inhibition of IL-10 production.

: U0126 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 28;430:201-214. [Abstract]; Inhibition of ERK suppresses N-cadherin expression. CD146^WT or CD146^KO MEFs are stimulated with or without TGF-β1 (10 ng/mL) for 24 h in the presence or absence of U0126 (2 μM). The expression and activation of ERK and the expression of E-cadherin and N-cadherin is assessed by immunoblotting.

: U0126 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291. [Abstract]; Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

: U0126 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291. [Abstract]; Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

: U0126 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184. [Abstract]; Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

: U0126 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Oct 3;9(10):1015. [Abstract]; Representative western blot images are showing the LC3, and the phosphorylated and total protein expression of Akt and ERK1/2 after treatment with H₂O₂ in the presence and absence of MK2206 (5 μM) and U0126 (25 μM).

: U0126 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269. [Abstract]; WB is used to detect the effect of EGF treatment on the expression of YAP with the inhibitors of EGFR or its downsream members.

: U0126 purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163. [Abstract]; Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Feb 19;100:417-425. [Abstract]; HaCaT cells are pre-incubated with Compound C (CC) (10 μM) and U0126 (10 μM), pharmacological inhibitors of AMPKα, ERK, respectively, for 1 h before treatment with DA8 and DA14 (DAs).

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

: U0126 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

: U0126 purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854. [Abstract]; Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

: U0126 purchased from MCE. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55. [Abstract]; Western blot analysis of claudin 5, occludin and ZO-1 in TM4 cells, cells are treated with 100 nM Leptin or pre-treated with different inhibitors following a 100 nM Leptin treatment.

: U0126 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Sep 19. [Abstract]; Western blot shows the expression of p-ERK and MMP13 with the treatment of U0126 and CCL17.

: U0126 purchased from MCE. Usage Cited in: Mol Med Rep. 2018 Jun;17(6):7595-7602. [Abstract]; Representative images show the expression levels of α SMA, calponin and osteopontin (OPN) protein.

: U0126 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;50(4):1522-1534. [Abstract]; Western analysis of effect of U0126 on Nell-1-induced changes in p-ERK, Runx2, OPG and Col-I protein expression in MC3T3-E1 preosteoblasts on Ti surfaces.

: U0126 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32. [Abstract]; Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

: U0126 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59. [Abstract]; Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

: U0126 purchased from MCE. Usage Cited in: Cell Signal. 2017 Jan 16;32:48-58. [Abstract]; Western blotting showing the hepaCAMexpression and the phosphorylation level of STAT3, ERK and AKT in cells treated with IL-6 (20 ng/mL) for 24 h with or without the pretreatment of two respective inhibitors, Stattic (10 μM) and U0126 (5 μM).

: U0126 purchased from MCE. Usage Cited in: Cell Cycle. 2017 Apr 3;16(7):714-722. [Abstract]; Proliferation of OPCs by AST induced calcium signaling and phosphorylated ERK1/2. p-ERK levels decreased after Cx47 siRNA treatment and U0126-mediated ERK1/2 inhibition. The results of Western blotting show that U0126 causes a marked decrease in ERK1/2 phosphorylation

: U0126 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 30;8(47):82027-82036. [Abstract]; U0126 and MEK162 block ERK activation (p-ERK1/2) in CZ415-treated U2OS cells.

: U0126 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 16;8(20):33807-33826. [Abstract]; U0126 inhibits ERK1/2 activation in the kidney of hyperuricemic rats. Rat model of HN is established by feeding with adenine and potassium oxonate daily. In some rats, U0126 are simultaneously administrated intraperitoneally. After 28 days, the kidneys are taken for immunoblot analysis of p-ERK1/2, ERK1/2 or GAPDH.

: U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458. [Abstract]; Representative immunoblot analysis of p53, p16, p21, and retinoblastoma protein (Rb) in NP cells.

: U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841. [Abstract]; Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with U0126 (an ERK1/2 inhibitor, 10 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

: U0126 purchased from MCE. Usage Cited in: ACS Chem Neurosci. 2015 Jan 21;6(1):130-7. [Abstract]; U0126 protects PC12 cells against H2O2-induced cell death. Western blot of ERK phosphorylation demonstrates that the MEK inhibitors U0126, GSK1120212 and Pimasertib are effective in blocking ERK phosphorylation under complete media, while U0124 results in slight ERK inhibition compared to DMSO control. Serum starvation results in lack of ERK phosphorylation in all conditions.

: U0126 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79. [Abstract]; Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

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生物活性
纯度 & 产品资料
参考文献

生物活性

U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]

MEK2

60 nM (IC₅₀)

MEK1

70 nM (IC₅₀)

体外研究
(In Vitro)

Treatment with U0126 efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126 are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126 are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC₅₀ values for U0126-EtOH against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells^[2].
Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126 strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G₀-G₁ phase and to a lesser extent in G₂/M^[3].

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

Cell Viability Assay^[2]

Cell Line:	A549 and MDCK II cells.
Concentration:	0.001-1000 μM.
Incubation Time:	48 h.
Result:	The EC₅₀ values for U0126 against H1N1v were 1.2 ± 0.4 μM in A549 cells and 74.7 ± 1.0 μM in MDCKII cells

体内研究
(In Vivo)

Mice are treated daily with U0126-EtOH (U0126; i.p., 10.5 mg/kg). In control experiment, tumor sizes are constant or slightly increase all over the kinetic. At the opposite, in all U0126-EtOH experiments, engraftment and early tumor growth are significantly decreased. Furthermore, a 60-70% reduction in the volume of tumors treated with U0126-EtOH is obtained 9 days after injection and thereafter^[3].
Rats are subjected to 120 minutes transient middle cerebral artery occlusion (tMCAO) and thereafter treated with the U0126-EtOH (U0126; i.p., 30 mg/kg) at 0 and 24 hours of reperfusion. After treatment with U0126-EtOH, the vasoconstriction to S6c is markedly reduced^[4].

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

Animal Model:	Athymic female nude mice (SWISS, nu/nu)^[3].
Dosage:	10.5 mg/kg.
Administration:	Intraperitoneal injection daily.
Result:	Inhibited tumor growth.

Animal Model:	Twelve-week-old female Wistar rats (250 to 265 g) ^[4].
Dosage:	30 mg/kg.
Administration:	Intraperitoneally.
Result:	The vasoconstriction to S6c is markedly reduced.

分子量

380.49

Formula

C₁₈H₁₆N₆S₂

CAS 号

109511-58-2

性状

固体

颜色

Off-white to light yellow

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (262.82 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6282 mL	13.1409 mL	26.2819 mL
5 mM	0.5256 mL	2.6282 mL	5.2564 mL
10 mM	0.2628 mL	1.3141 mL	2.6282 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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 (6.57 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 (6.57 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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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 (6.57 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: 98.45%

选择批次：

Data Sheet (627 KB) SDS (251 KB)

COA (286 KB) HNMR (275 KB) LCMS (100 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Favata MF, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32. [Content Brief]

[2]. Droebner K, et al. Antiviral activity of the MEK-inhibitor U0126 against pandemic H1N1v and highly pathogenic avian influenza virus in vitro and in vivo. Antiviral Res. 2011, 92(2), 195-203. [Content Brief]

[3]. Bessard A, et al. RNAi-mediated ERK2 knockdown inhibits growth of tumor cells in vitro and in vivo. Oncogene. 2008 Sep 11;27(40):5315-25. [Content Brief]

[4]. Ahnstedt H, et al. U0126 attenuates cerebral vasoconstriction and improves long-term neurologic outcome after stroke in female rats. J Cereb Blood Flow Metab. 2015 Mar;35(3):454-60. [Content Brief]

U0126 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	2.6282 mL	13.1410 mL	26.2819 mL	65.7048 mL
	5 mM	0.5256 mL	2.6282 mL	5.2564 mL	13.1410 mL
	10 mM	0.2628 mL	1.3141 mL	2.6282 mL	6.5705 mL
	15 mM	0.1752 mL	0.8761 mL	1.7521 mL	4.3803 mL
	20 mM	0.1314 mL	0.6570 mL	1.3141 mL	3.2852 mL
	25 mM	0.1051 mL	0.5256 mL	1.0513 mL	2.6282 mL
	30 mM	0.0876 mL	0.4380 mL	0.8761 mL	2.1902 mL
	40 mM	0.0657 mL	0.3285 mL	0.6570 mL	1.6426 mL
	50 mM	0.0526 mL	0.2628 mL	0.5256 mL	1.3141 mL
	60 mM	0.0438 mL	0.2190 mL	0.4380 mL	1.0951 mL
	80 mM	0.0329 mL	0.1643 mL	0.3285 mL	0.8213 mL
	100 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6570 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:

U0126109511-58-2U 0126U-0126MEKAutophagyMitophagyInfluenza VirusMitogen-activated protein kinase kinaseMAPKKMAP2KMitochondrial AutophagyInhibitorinhibitorinhibit

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U0126

Customer Review

Other Forms of U0126:

MCE 顾客使用本产品发表的 360 篇科研文献

U0126 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 MEK 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

U0126 相关分类

完整储备液配制表

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U0126

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