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Chemical Structure| 1173097-76-1 Chemical Structure| 1173097-76-1

Structure of U0126-EtOH
CAS No.: 1173097-76-1

Chemical Structure| 1173097-76-1

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U0126 (U0126-EtOH) is a potent, non-ATP competitive, and selective MEK1 and MEK2 inhibitor with IC50 values of 72 nM and 58 nM, respectively. It also inhibits autophagy and mitophagy.

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Product Details of U0126-EtOH

CAS No. :1173097-76-1
Formula : C20H22N6OS2
M.W : 426.56
SMILES Code : N#CC(/C(C#N)=C(N)/SC1=CC=CC=C1N)=C(N)\SC2=CC=CC=C2N.CCO
MDL No. :MFCD22628895
InChI Key :CFQULUVMLGZVAF-OYJDLGDISA-N
Pubchem ID :16220066

Safety of U0126-EtOH

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of U0126-EtOH

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK2

    MEK2, IC50:0.06 μM

  • MEK1

    MEK1, IC50:0.07 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
MEL10 cells 10 µM 5 days U0126 induced cyclin D1-negative senescence. PMC3741510
HT-p16 cells 10 µM 24 h U0126 completely eliminated cyclin D1 accumulation, making it undetectable. PMC3741510
HT-p21 cells 10 µM 24 h U0126 completely eliminated cyclin D1 accumulation, making it undetectable. PMC3741510
TE671 cells 40 μM 7 days U0126 significantly reduced the number of CD133 and CXCR4 positive cells in TE671 cells and inhibited rhabdosphere formation. PMC4761200
RD cells 10 μM 15 days Inhibition of the MEK/ERK pathway in RD cells significantly reduced rhabdosphere formation and downregulated the expression of stem cell markers CD133, CXCR4, and Nanog, while enhancing ALDH, MAPK p38, and differentiative myogenic markers. PMC4761200
Canine tracheal smooth muscle cells 15 μM or 30 μM ≥45 min U0126 increased the force-fluctuation-induced relengthening (FFIR) of acetylcholine-contracted canine tracheal smooth muscle strips in a concentration-dependent manner, and this effect was negatively correlated with the phosphorylation of high-molecular-weight caldesmon (h-caldesmon). PMC3918254
Mouse primary cultured cortical neurons 10 µM 24 h U0126 inhibited neuronal cell death, protecting cortical neurons against oxygen deprivation. PMC58770

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice Embryonal rhabdomyosarcoma model Intraperitoneal injection 25 μM/kg 3 times per week for 4 weeks Intraperitoneal administration of U0126 significantly inhibited tumor growth induced by rhabdosphere cells, delayed tumor progression time, and reduced tumor volume. PMC4761200
Gerbils Forebrain ischemia model I.v. administration 100 mg/kg Single injection, 10 min before ischemia U0126 reduced the loss of CA1 pyramidal cells at 7 days, protecting the hippocampus against forebrain ischemia. PMC58770

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL

References

 

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