U-0126__MEK inhibitor BYL-721
Product Name
U-0126
Description
MEK inhibitor
Purity
>98%
CAS No.
109511-58-2
Molecular Formula
C18H16N6S2
Molecular Weight
380.5
Storage Temperature
-20ºC
Shipping Temperature
Shipped Ambient
Product Type
Inhibitor
Solubility
Soluble in DMSO (>10 mg/ml), 100% ethanol (2 mg/ml)
Source
Synthetic
Appearance
White solid
SMILES
C2=C(SC(/N)=C(/C(=C(SC1=CC=CC=C1N)N)C#N)C#N)C(=CC=C2)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+
InChIKey
DVEXZJFMOKTQEZ-JYFOCSDGSA-N
Safety Phrases
Classification: Caution: Substance not yet fully tested.
Safety Phrases:
S22 – Do not breathe dust.
S24/25 – Avoid contact with skin and eyes
S36/37/39 – Wear suitable protective clothing, gloves and eye/face protection
Cite This Product
U-0126 (StressMarq Biosciences Inc., Victoria BC CANADA, Catalog # SIH-380)
Alternative Names
1,4-Diamino-2,3-dicyano-1,4-bis2-aminophenylthiobutadiene
Research Areas
Cell Signaling
PubChem ID
3006531
Scientific Background
U-0126 is a novel, potent and selective MEK inhibitor (MEK1; IC50=72nM, MEK2; IC50=58nM). Inhibits AP-1 transcription activity. Blocks the production of inflammatory cytokines and matrix metalloproteinases.
Binding of extracellular growth factors to cell surface receptors often results in activation of the mitogen-activated protein kinase (MAPK). MAPK is regulated by MAPK kinase, also called MEK. Deprivation of growth factors during cell culture or intracellular MEK inhibition leads to inhibition of proliferation and apoptotic cell death. N Blank et al. (2002) have shown that U0126, a common used MEK inhibitor and compound that itself has no intrinsic fluorescence in vitro but develops an intensive fluorescence during cell culture which can be observed in all fluorescence channels with predominance in the FL1 channel (525nm).
References
1. Duncia J.V., et a.l (1998) Bioorg. Med. Chem. Lett. 8(20): 2839-44.
2. Favata M.F., et al. (1998) J. Biol. Chem. 273(29): 18623-32.
3. Davies S.P., et al. (2000) Biochem. J. 351(Pt1): 95-105.
4. Namura S., et al. (2001) Proc. Natl. Acad. Sci. U.S.A. 98(20): 11569-74.
MEK inhibitor
Safety Phrases:
S22 – Do not breathe dust.
S24/25 – Avoid contact with skin and eyes
S36/37/39 – Wear suitable protective clothing, gloves and eye/face protection
Binding of extracellular growth factors to cell surface receptors often results in activation of the mitogen-activated protein kinase (MAPK). MAPK is regulated by MAPK kinase, also called MEK. Deprivation of growth factors during cell culture or intracellular MEK inhibition leads to inhibition of proliferation and apoptotic cell death. N Blank et al. (2002) have shown that U0126, a common used MEK inhibitor and compound that itself has no intrinsic fluorescence in vitro but develops an intensive fluorescence during cell culture which can be observed in all fluorescence channels with predominance in the FL1 channel (525nm).
2. Favata M.F., et al. (1998) J. Biol. Chem. 273(29): 18623-32.
3. Davies S.P., et al. (2000) Biochem. J. 351(Pt1): 95-105.
4. Namura S., et al. (2001) Proc. Natl. Acad. Sci. U.S.A. 98(20): 11569-74.