U0126


Catalog No. Size PriceQuantity
M7704-2 2mg solid $85
M7704-10 10mg solid $255

Description

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).

Product information

CAS Number: 109511-58-2

Molecular Weight: 380.49

Formula: C18H16N6S2

Synonym:

U 0126

Related CAS Number:

1173097-76-1 (U0126-EtOH)

Chemical Name: (2Z, 3Z)-2, 3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile

Smiles: NC1=CC=CC=C1SC(N)=C(C#N)C(C#N)=C(N)SC1=CC=CC=C1N

InChiKey: DVEXZJFMOKTQEZ-JYFOCSDGSA-N

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+

Technical Data

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

In Vitro:

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.

In Vivo:

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.

References:

  1. Freeman MR, et al. Cancer Biol Ther. 2011, 12(11), 966-977.
  2. DeSilva DR, et al. J Immunol. 1998, 160(9), 4175-4181.
  3. Duncia JV, et al. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844.

Products are for research use only. Not for human use.

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