WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H462848
CAS#: 218601-62-8
Description: U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways.
Hodoodo Cat#: H462848
Name: U-0126
CAS#: 218601-62-8
Chemical Formula: C18H16N6S2
Exact Mass: 380.09
Molecular Weight: 380.488
Elemental Analysis: C, 56.82; H, 4.24; N, 22.09; S, 16.85
Related CAS #: 218601-62-8; 109511-58-2;
Synonym: U0126; U-0126;
IUPAC/Chemical Name: (2Z,3Z)-2,3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile
InChi Key: DVEXZJFMOKTQEZ-JYFOCSDGSA-N
InChi Code: InChI=1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+
SMILES Code: N/C(Sc1c(N)cccc1)=C(\C(C#N)=C(Sc2c(N)cccc2)/N)C#N
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 380.49 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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5: Li T, Hu J, Gao F, Du X, Chen Y, Wu Q. Transcription factors regulate GPR91-mediated expression of VEGF in hypoxia-induced retinopathy. Sci Rep. 2017 Apr 4;7:45807. doi: 10.1038/srep45807. PMID: 28374767; PMCID: PMC5379554.
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7: Wang A, Zhang H, Liang Z, Xu K, Qiu W, Tian Y, Guo H, Jia J, Xing E, Chen R, Xiang Z, Liu J. U0126 attenuates ischemia/reperfusion-induced apoptosis and autophagy in myocardium through MEK/ERK/EGR-1 pathway. Eur J Pharmacol. 2016 Oct 5;788:280-285. doi: 10.1016/j.ejphar.2016.06.038. Epub 2016 Jun 23. PMID: 27343376.
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13: Tao M, Shi Y, Tang L, Wang Y, Fang L, Jiang W, Lin T, Qiu A, Zhuang S, Liu N. Blockade of ERK1/2 by U0126 alleviates uric acid-induced EMT and tubular cell injury in rats with hyperuricemic nephropathy. Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F660-F673. doi: 10.1152/ajprenal.00480.2018. Epub 2019 Jan 16. PMID: 30648910; PMCID: PMC6483027.
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15: Ji Q, Wang YL, Xia LM, Yang Y, Wang CS, Mei YQ. High shear stress suppresses proliferation and migration but promotes apoptosis of endothelial cells co- cultured with vascular smooth muscle cells via down-regulating MAPK pathway. J Cardiothorac Surg. 2019 Dec 12;14(1):216. doi: 10.1186/s13019-019-1025-5. PMID: 31831023; PMCID: PMC6909635.
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