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Submit ReviewU0126 is a potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Brain penetrant. Helps maintain human pluripotent stem cells in undifferentiated state.
Negative Control also available.
分子量 | 380.48 |
公式 | C18H16N6S2 |
储存 | Desiccate at +4°C |
CAS Number | 109511-58-2 |
PubChem ID | 3006531 |
InChI Key | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
Smiles | N\C(SC1=CC=CC=C1N)=C(C#N)/C(C#N)=C(\N)SC1=CC=CC=C1N |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.05 | 100 |
以下数据基于产品分子量 380.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.63 mL | 13.14 mL | 26.28 mL |
5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Duncia et al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg.Med.Chem.Lett. 8 2839 PMID: 9873633
Favata et al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J.Biol.Chem. 273 18623 PMID: 9660836
Namura et al (2001) Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc.Natl.Acad.Sci.U.S.A. 98 11569 PMID: 11504919
Kinehara et al (2013) Protein kinase C regulates human pluripotent stem cell self-renewal. PLoS One 8 e54122 PMID: 23349801
If you know of a relevant reference for U0126, please let us know.
关键词: U0126, U0126 supplier, Potent, selective, inhibitors, inhibits, MEK1, MEK2, Mitogen-Activated, Protein, Kinase, Kinases, MEK, Stem, Cell, Proliferation, 1144, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 U0126 的部分引用包括:
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To investigate if the induction of Snail1 by Helicobacter pylori infection in gastric epithelial cells AGS was regulated by the MEK/ERK pathway.
Aliquot the reconstituted compound to avoid freezing and thawing repeatedly.
Pancreatic cancer cells were pretreated for 2 hours with U0126 followed by conventional chemotherapeutics. MEK inhibition had an additive effect on cancer cell’s viability upon 3 days of treatment.
All MAPK inhibitors (ZM336372: c-RAF inhibitor; UO126: MEK1/MEK2 inhibitor, SB203580: p38 inhibitor) were used at 10 μM
We ordered this product, combining with another inhibitor, to confirm the migration.To confirm that tested product induces migration, we also screen all MAPK inhibitors and MIF receptor antagonists
Extracellular flux analysis (Seahorse experiment) to examine the effect of MEK inhibitor in breast cancer cells. 5-10uM dose used.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.