Date published: 2025-12-17

1-800-457-3801

SCBT Portrait Logo
Seach Input

U-0126 (CAS 109511-58-2)

5.0(2)
Write a reviewAsk a question

See product citations (136)

Alternate Names:
U-0126 is known as an MEK inhibitor and AMPK activator.
Application:
U-0126 is a highly selective, non-ATP competitive MAP Kinase Kinase (MKK, MEK1 and MEK2) and ERK inhibitor.
CAS Number:
109511-58-2
Purity:
≥97%
Molecular Weight:
380.48
Molecular Formula:
C18H16N6S2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

QUICK LINKS

U-0126 is a selective MAPK and ERK inhibitor, displaying a preference for MEK1 and MEK2. The IC50 value for MEK1 is 72nM and MEK2 is 58nM. It is known that U-0126 binds to MAPK noncompetitive manner compared to ATP. Studies suggest that U-0126 antagonizes the transcription of AP-1, via the inhibition of MEK. In addition, U-0126 has been observed to inhibit promoters containing an AP-1 response element. Conversely, U-0126 has no effect on promoters that lack an AP-1 response group. U-0126 is also useful in neuronal studies in mice since it displays inhibitory effects against oxidative stress.


U-0126 (CAS 109511-58-2) References

  1. Neuroprotection by MAPK/ERK kinase inhibition with U0126 against oxidative stress in a mouse neuronal cell line and rat primary cultured cortical neurons.  |  Satoh, T., et al. 2000. Neurosci Lett. 288: 163-6. PMID: 10876086
  2. Extracellular regulated protein kinases play a key role via bone morphogenetic protein 4 in high phosphate-induced endothelial cell apoptosis.  |  Qin, L., et al. 2015. Life Sci. 131: 37-43. PMID: 25896660
  3. Dopamine D1 receptor-mediated activation of the ERK signaling pathway is involved in the osteogenic differentiation of bone mesenchymal stem cells.  |  Wang, CX., et al. 2020. Stem Cell Res Ther. 11: 12. PMID: 31900224
  4. The physiological modulation by intracellular kinases of hippocampal γ-oscillation in vitro.  |  Wang, J., et al. 2020. Am J Physiol Cell Physiol. 318: C879-C888. PMID: 32023074
  5. Dual blockade of protease-activated receptor 1 and 2 additively ameliorates diabetic kidney disease.  |  Mitsui, S., et al. 2020. Am J Physiol Renal Physiol. 318: F1067-F1073. PMID: 32200667
  6. Comparative proteomic analysis to identify the novel target gene of angiotensin II in adrenocortical H295R cells.  |  Ito, R., et al. 2021. Endocr J. 68: 441-450. PMID: 33390420
  7. DHEA inhibits proliferation, migration and alters mesenchymal-epithelial transition proteins through the PI3K/Akt pathway in MDA-MB-231 cells.  |  Colín-Val, Z., et al. 2021. J Steroid Biochem Mol Biol. 208: 105818. PMID: 33508440
  8. Myeloid cell-derived coagulation tissue factor is associated with renal tubular damage in mice fed an adenine diet.  |  Yamakage, S., et al. 2021. Sci Rep. 11: 12159. PMID: 34108522
  9. Tingenone and 22-hydroxytingenone target oxidative stress through downregulation of thioredoxin, leading to DNA double-strand break and JNK/p38-mediated apoptosis in acute myeloid leukemia HL-60 cells.  |  Rodrigues, ACBDC., et al. 2021. Biomed Pharmacother. 142: 112034. PMID: 34411914
  10. Benzyl Isothiocyanate Attenuates Inflammasome Activation in Pseudomonas aeruginosa LPS-Stimulated THP-1 Cells and Exerts Regulation through the MAPKs/NF-κB Pathway.  |  Park, WS., et al. 2022. Int J Mol Sci. 23: PMID: 35163151
  11. Selective Δ-Opioid Receptor Agonist, KNT-127, Facilitates Contextual Fear Extinction via Infralimbic Cortex and Amygdala in Mice.  |  Kawaminami, A., et al. 2022. Front Behav Neurosci. 16: 808232. PMID: 35264937
  12. Lysophosphatidylinositol Induced Morphological Changes and Stress Fiber Formation through the GPR55-RhoA-ROCK Pathway.  |  Nakajima, K., et al. 2022. Int J Mol Sci. 23: PMID: 36142844
  13. Multi-Omics Immune Interaction Networks in Lung Cancer Tumorigenesis, Proliferation, and Survival.  |  Ye, Q., et al. 2022. Int J Mol Sci. 23: PMID: 36499305
  14. Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes.  |  Scherle, PA., et al. 1998. J Immunol. 161: 5681-6. PMID: 9820549
  15. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.  |  Duncia, JV., et al. 1998. Bioorg Med Chem Lett. 8: 2839-44. PMID: 9873633

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

U-0126, 1 mg

sc-222395
1 mg
$63.00

U-0126, 5 mg

sc-222395A
5 mg
$241.00