U0126 is a potent and selective non-competitive inhibitor of MAP kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively).
CAS Number: 109511-58-2
Molecular Weight: 380.49
Related CAS Number:
Chemical Name: (2Z, 3Z)-2, 3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 85 mg/mLwarmed(199.26 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels. A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK.
U0126-EtOH, as the inhibitor of intracellular Raf/MEK/ERK signaling pathway, demonstrates antiviral activity by suppressing propagation of the 2009 pandemic IV H1N1 variant and highly pathogenic avian influenza viruses (HPAIV) in vivo in the mouse lung by inhibiting. U0126-EtOH shows the potential neuroprotective effect and improving spatial learning in Morris water maze (MWM) by activating peroxisome proliferator-activated receptor gamma coactivator-1a, nuclear respiratory factor 1, and mitochondrial transcription factor A in Aβ-injected rats.
- Freeman MR, et al. Cancer Biol Ther. 2011, 12(11), 966-977.
- DeSilva DR, et al. J Immunol. 1998, 160(9), 4175-4181.
- Duncia JV, et al. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844.
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