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U 0126
- U 126
- Soluble in DMSO and EtOH
- MF: C18H16N6S2
- MW: 380.49
Description
U 0126 is a noncompetitive inhibitor of MEK1 and MEK2, the dual-specificity kinases upstream of ERK1/2. It suppresses MAPK/ERK pathway activation without directly inhibiting ERK catalytic activity.
MEK1/2 signaling controls proliferation, differentiation, survival and stress responses downstream of RAS and RAF. U 0126 is a benchmark MEK inhibitor for dissecting ERK pathway dependency in cellular and in vivo models.
Key Features
- MEK1/2 inhibitor
- Reported IC50 values: 0.07 µM for MEK1 and 0.06 µM for MEK2
- Noncompetitive inhibition profile
- Blocks ERK pathway activation downstream of RAF
Applications
- MAPK/ERK signaling research
- Cell proliferation and differentiation studies
- Neuroprotection and ischemia pathway models
- MEK inhibitor assay controls
More Information
| Parent CAS No. | 109511-58-2 |
|---|---|
| Chemical Name | 2,3-bis(amino(2-aminophenylthio)methylene)succinonitrile |
| SMILES | C(#N)/C(=C(/N)SC1=CC=CC=C1N)/C(=C(N)/SC1=CC=CC=C1N)/C#N |
| MFCD | MFCD25977152 |
| InChi | 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+ |
| InChiKey | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
| CID | 3006531 |
| Short Description | MEK1/2 inhibitor |
References
- J.V. Duncia et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44.
- H. Hotokezaka et al. U0126 and PD98059, specific inhibitors of MEK, accelerate differentiation of RAW264.7 cells into osteoclast-like cells. J Biol Chem. 2002 Dec 6;277(49):47366-72.
- M.F. Favata et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32.
- S. Namura et al. Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc Natl Acad Sci U S A. 2001 Sep 25;98(20):11569-74.
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