Molecular structure of MEK Inhibitor I, CAS Number: 297744-42-4
MEK Inhibitor I (CAS 297744-42-4)
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Application:
MEK Inhibitor I is a vinylogous cyanamide that has the ability to act as a selective and potent inhibitor of MEK
CAS Number:
297744-42-4
Purity:
≥95%
Molecular Weight:
374.46
Molecular Formula:
C21H18N4OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
MEK Inhibitor I is a cell-permeable, pyridine-containing, vinylogous cyanamide that has the ability to act as a selective and potent inhibitor of MEK with little activity towards MKK3 and MKK4. The compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP) and the demonstrated inhibition is noncompetitive with respect to ERK. Compared to U0126 in aqueous solutionsMEK Inhibitor I demonstrates superior potency, solubility, and stability. Additionally shown to protect against phorbol ester-mediated ear edema in mice.
MEK Inhibitor I (CAS 297744-42-4) References
- Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors. | Wityak, J., et al. 2004. Bioorg Med Chem Lett. 14: 1483-6. PMID: 15006386
- HTS assays using a disease-relevant cell model for interrogating the MAP kinase pathway initiated by multiple receptors. | Wilkinson, JM., et al. 2008. Assay Drug Dev Technol. 6: 351-9. PMID: 18593376
- Activation of a PAK-MEK signalling pathway in malaria parasite-infected erythrocytes. | Sicard, A., et al. 2011. Cell Microbiol. 13: 836-45. PMID: 21371233
- cAMP activates TRPC6 channels via the phosphatidylinositol 3-kinase (PI3K)-protein kinase B (PKB)-mitogen-activated protein kinase kinase (MEK)-ERK1/2 signaling pathway. | Shen, B., et al. 2011. J Biol Chem. 286: 19439-45. PMID: 21487005
- Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation. | Ripple, MO., et al. 2013. J Biol Chem. 288: 2933-40. PMID: 23235157
- Phosphoproteomics of MAPK inhibition in BRAF-mutated cells and a role for the lethal synergism of dual BRAF and CK2 inhibition. | Parker, R., et al. 2014. Mol Cancer Ther. 13: 1894-906. PMID: 24825855
- The MEK1/2 inhibitor, MEKi-1, induces cell death in chronic lymphocytic leukemia cells under conditions that mimic the tumor microenvironment and is synergistic with fludarabine. | Crassini, K., et al. 2015. Leuk Lymphoma. 56: 3407-17. PMID: 25804768
- Small molecules modulating tumor-stromal cell interactions: new candidates for anti-tumor drugs. | Kawada, M. 2016. J Antibiot (Tokyo). 69: 411-4. PMID: 27005556
- Trametinib Induces Neurofibroma Shrinkage and Enables Surgery. | Vaassen, P., et al. 2019. Neuropediatrics. 50: 300-303. PMID: 31141829
- Slowly progressive cell death induced by GPx4-deficiency occurs via MEK1/ERK2 activation as a downstream signal after iron-independent lipid peroxidation. | Tsuruta, K., et al. 2024. J Clin Biochem Nutr. 74: 97-107. PMID: 38510679
Inhibitor of:
MEK.Activator of:
Rheb.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
MEK Inhibitor I, 1 mg | sc-353669 | 1 mg | $218.00 |