U-0126
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MedKoo CAT#: 462848

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.


Chemical Structure

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U-0126
CAS# 218601-62-8

Theoretical Analysis

MedKoo Cat#: 462848
Name: U-0126
CAS#: 218601-62-8
Chemical Formula: C18H16N6S2
Exact Mass: 380.0878
Molecular Weight: 380.488
Elemental Analysis: C, 56.82; H, 4.24; N, 22.09; S, 16.85

Price and Availability

Size Price Availability Quantity
5.0mg USD 280.0 2 Weeks
10.0mg USD 470.0 2 Weeks
25.0mg USD 760.0 2 Weeks
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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

Preparing Stock Solutions

The following data is based on the product molecular weight 380.488 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.

Recalculate based on batch purity %
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

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1: Boyd DF, Mathie A. Inhibition of the potassium current IK(SO), in cerebellar granule cells, by the inhibitors of MEK1 activation, PD 98059 and U 0126. Neuropharmacology. 2002 Feb;42(2):221-8. doi: 10.1016/s0028-3908(01)00168-x. PMID: 11804618.

2: Aimond F, Fauconnier J, Donadille D, Vassort G. The p42/44mitogen-activated protein kinase inhibitor PD 98059, but not U 0126, increases a K+ current in cardiomyocytes. Clin Exp Pharmacol Physiol. 2003 Apr;30(4):273-7. doi: 10.1046/j.1440-1681.2003.03826.x. PMID: 12680846.

3: Liao Q, Qu S, Tang LX, Li LP, He DF, Zeng CY, Wang WE. Irisin exerts a therapeutic effect against myocardial infarction via promoting angiogenesis. Acta Pharmacol Sin. 2019 Oct;40(10):1314-1321. doi: 10.1038/s41401-019-0230-z. Epub 2019 May 6. PMID: 31061533; PMCID: PMC6786355.

4: Shahidullah M, Mandal A, Delamere NA. Activation of TRPV1 channels leads to stimulation of NKCC1 cotransport in the lens. Am J Physiol Cell Physiol. 2018 Dec 1;315(6):C793-C802. doi: 10.1152/ajpcell.00252.2018. Epub 2018 Sep 12. PMID: 30207782; PMCID: PMC6336939.

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.

6: Kim HK, Lim S, Bae MJ, Lee W, Kim S. PG102 Upregulates IL-37 through p38, ERK, and Smad3 Pathways in HaCaT Keratinocytes. Mediators Inflamm. 2019 Feb 24;2019:6085801. doi: 10.1155/2019/6085801. PMID: 30918469; PMCID: PMC6409045.

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.

8: Jeon J, Kwon H, Cho E, Kim KS, Yun J, Lee YC, Kim DH. The effect of coniferaldehyde on neurite outgrowth in neuroblastoma Neuro2a cells. Neurochem Int. 2019 Dec;131:104579. doi: 10.1016/j.neuint.2019.104579. Epub 2019 Oct 12. PMID: 31614166.

9: Yano S, Wu S, Sakao K, Hou DX. Involvement of ERK1/2-mediated ELK1/CHOP/DR5 pathway in 6-(methylsulfinyl)hexyl isothiocyanate-induced apoptosis of colorectal cancer cells. Biosci Biotechnol Biochem. 2019 May;83(5):960-969. doi: 10.1080/09168451.2019.1574206. Epub 2019 Feb 7. PMID: 30730256.

10: Liu X, Lin L, Li Q, Ni Y, Zhang C, Qin S, Wei J. ERK1/2 communicates GPCR and EGFR signaling pathways to promote CTGF-mediated hypertrophic cardiomyopathy upon Ang-II stimulation. BMC Mol Cell Biol. 2019 Jun 14;20(1):14. doi: 10.1186/s12860-019-0202-7. PMID: 31200637; PMCID: PMC6570861.

11: Fu R, Wang X, Hu Y, Du H, Dong B, Ao S, Zhang L, Sun Z, Zhang L, Lv G, Ji J. Solamargine inhibits gastric cancer progression by regulating the expression of lncNEAT1_2 via the MAPK signaling pathway. Int J Oncol. 2019 May;54(5):1545-1554. doi: 10.3892/ijo.2019.4744. Epub 2019 Mar 12. PMID: 30864686; PMCID: PMC6438418.

12: Mandl M, Wagner SA, Hatzmann FM, Mitterberger-Vogt MC, Zwierzina ME, Mattesich M, Zwerschke W. Sprouty1 is a weight-loss target gene in human adipose stem/progenitor cells that is mandatory for the initiation of adipogenesis. Cell Death Dis. 2019 May 28;10(6):411. doi: 10.1038/s41419-019-1657-3. PMID: 31138786; PMCID: PMC6538615.

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.

14: Sikorska J, Gaweł D, Domek H, Rudzińska M, Czarnocka B. Podoplanin (PDPN) affects the invasiveness of thyroid carcinoma cells by inducing ezrin, radixin and moesin (E/R/M) phosphorylation in association with matrix metalloproteinases. BMC Cancer. 2019 Jan 17;19(1):85. doi: 10.1186/s12885-018-5239-z. PMID: 30654768; PMCID: PMC6337816.

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.

16: Lan CE, Wu CS, Huang SM, Wu CH, Lai HC, Peng YT, Hou PS, Yang HJ, Chen GS. Irradiance-dependent UVB Photocarcinogenesis. Sci Rep. 2016 Nov 21;6:37403. doi: 10.1038/srep37403. PMID: 27869214; PMCID: PMC5116611.

17: Lall MM, Harned J, McGahan MC. Hydrogen peroxide and extracellular signal- related kinase 1/2 pathway regulate ferritin levels in retinal pigmented and lens epithelial cells. Mol Vis. 2013 Oct 4;19:2106-12. PMID: 24146543; PMCID: PMC3800279.

18: Chen T, Bi K, Zhao Y, Lyu X, Gao Z, Zhao Y, Fu Y, Cheng J, Xie J, Jiang D. MAPKK Inhibitor U0126 Inhibits Plasmodiophora brassicae Development. Phytopathology. 2018 Jun;108(6):711-720. doi: 10.1094/PHYTO-07-17-0240-R. Epub 2018 May 7. PMID: 29381451.

19: House SL, Branch K, Newman G, Doetschman T, Schultz Jel J. Cardioprotection induced by cardiac-specific overexpression of fibroblast growth factor-2 is mediated by the MAPK cascade. Am J Physiol Heart Circ Physiol. 2005 Nov;289(5):H2167-75. doi: 10.1152/ajpheart.00392.2005. Epub 2005 Jul 22. PMID: 16040717.

20: Kling DE, Lorenzo HK, Trbovich AM, Kinane TB, Donahoe PK, Schnitzer JJ. MEK-1/2 inhibition reduces branching morphogenesis and causes mesenchymal cell apoptosis in fetal rat lungs. Am J Physiol Lung Cell Mol Physiol. 2002 Mar;282(3):L370-8. doi: 10.1152/ajplung.00200.2001. PMID: 11839529.

U-0126

5.0mg / USD 280.0