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U0126, 10 mg  

U0126, 10 mg

1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene

Synonyms: UO 126, U0-126
selective inhibitor of MEK-1 and MEK-2

More details

PKI-U0126-010

Availability: on stock

136,50 €

Background: U0126 is a selective inhibitor of the mitogen-activated protein kinase kinases, MEK-1 and MEK-2, with a 100-fold higher potency than PD 98059. It is a weak inhbitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4 and inhibits AP-1 transactivation in cell-based reporter assays.

Molecular weight: 380.5 g/mol
Chemical formula: C18H16N6S2
Solubility: Soluble in DMSO
Purity: >98%
CAS Number: 109511-58-2

Product specific literature references:

Duncia JV, Santella JB 3rd, Olson RE et al. (1998) "MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products" Bioorg. Med. Chem. Lett. 8(20):2839-44

Satoh T, Nakatsuka D, Namura S et al. (2000) "Neuroprotection by MAPK/ERK kinase inhibition with U0126 against oxidative stress in a mouse neuronal cell line and rat primary cultured cortical neurons" Neurosci. Lett. 288(2):163-6

Newton R, Cambridge L, Barnes PJ et al. (2000) "The MAP kinase inhibitors, PD098059, UO126 and SB203580, inhibit IL-1beta-dependent PGE(2) release via mechanistically distinct processes" Br. J. Pharmacol. 130(6):1353-61

Strohm C, Barancik T, Bruhl ML, Kilian SA, Schaper W (2000) "Inhibition of the ER-kinase cascade by PD98059 and UO126 counteracts ischemic preconditioning in pig myocardium" J. Cardiovasc. Pharmacol. 36(2):218-29

Namura S, Iihara K, Alessandrini A et al. (2001) "Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia" Proc. Natl. Acad. Sci. U S A. 98(20):11569-74

Wang X, Studzinski GP (2001) "Phosphorylation of raf-1 by kinase suppressor of ras is inhibited by "MEK-specific" inhibitors PD 098059 and U0126 in differentiating HL60 cells" Exp. Cell Res.268(2):294-300

Hotokezaka H, Sakai E, Nakayama K et al. (2002) "U0126 and PD98059, specific inhibitors of MEK, accelerate differentiation of RAW264.7 cells into osteoclast-like cells" J. Biol. Chem. 277(49):47366-72

Opavsky MA, Martino T, Liu PP et al. (2002) "Enhanced ERK-1/2 activation in mice susceptible to coxsackievirus-induced myocarditis" J. Clin. Invest. 109(12):1561-9

Niiya M, Niiya K, Tanimoto M et al. (2004) "Involvement of ERK1/2 and p38 MAP kinase in doxorubicin-induced uPA expression in human RC-K8 lymphoma and NCI-H69 small cell lung carcinoma cells" Oncology 67(3-4):310-9