U0126

Catalog #:

Synonyms: U0126

IUPAC Name:

Functional Activity:

U0126 is an inhibitor of both MEK1(IC₅₀ of 72 nM) and MEK2(IC₅₀ of 58 nM).

U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 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 (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways.

The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.

Technical Data:

M.Wt: 426.56

Formula: C₁₈H₁₆ N₆S₂.C₂ H₆O

Solubility: Soluble to 100 mM in DMSO

Purity: >97%

Storage: Dessicate at 4 degree C

CAS No.: 109511-58-2

Related Products by Target:

References for U0126:

1. Miwa, M., Uchida, S., Horiba, F., Takeshima, H., Nabeshima, T., and Hiramatsu, M. Nociceptin and its metabolite attenuate U0126-induced memory impairment through a nociceptin opioid peptide (NOP) receptor-independent mechanism. Neurobiol Learn Mem, 93: 396-405.

2. Zhao, L. Y., Huang, C., Li, Z. F., Liu, L., Ni, L., and Song, T. S. STAT1/2 is involved in the inhibition of cell growth induced by U0126 in HeLa cells. Cell Mol Biol (Noisy-le-grand), 55 Suppl: OL1168-1174, 2009.

3. Chen, C. L., Li, T. P., and Zhu, L. H. [Effect of MAPK signal transduction pathway inhibitor U0126 on aquaporin 4 expression in alveolar type II cells in rats with oleic acid-induced acute lung injury]. Nan Fang Yi Ke Da Xue Xue Bao, 29: 1525-1528, 2009.

4. Quan, H., Liu, H., Li, C., and Lou, L. 1,4-Diamino-2,3-dicyano-1,4-bis(methylthio)butadiene (U0126) enhances the cytotoxicity of combretastatin A4 independently of mitogen-activated protein kinase kinase. J Pharmacol Exp Ther, 330: 326-333, 2009.

5. Marampon, F., Bossi, G., Ciccarelli, C., Di Rocco, A., Sacchi, A., Pestell, R. G., and Zani, B. M. MEK/ERK inhibitor U0126 affects in vitro and in vivo growth of embryonal rhabdomyosarcoma. Mol Cancer Ther, 8: 543-551, 2009.

6. Yao, X. L., Chen, Z. D., Tan, F. Q., Lu, Y., and Hu, Q. [Protective effect of MEK inhibitor (U0126) on donor testes from ischemia-reperfusion injury after orthotopic testicular transplantation in rats]. Zhejiang Da Xue Xue Bao Yi Xue Ban, 38: 81-88, 2009.

Certificate of Analysis/MSDS is available upon request with lot number