Description
Key facts
CAS number:305350-87-2,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:335.3 Da,
Molecular formula:C16H12F3N3S,
PubChem:9549284,
Nature:Synthetic,
Solubility:Soluble in DMSO to 100 mMSoluble in ethanol to 100 mM (with heating),
Biochemical name:alpha-[Amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitrile,
Biological description:Centrally active, brain penetrant selective MEK1 and MEK2 inhibitor (IC50 values in in vitro assays are 0.18 and 0.22 μM, respectively).,
Canonical smiles:C1=CC=C(C(=C1)C(=C(N)SC2=CC=C(C=C2)N)C#N)C(F)(F)F,
Isomeric smiles:C1=CC=C(C(=C1)/C(=C(\N)/SC2=CC=C(C=C2)N)/C#N)C(F)(F)F,
InChi:InChI=1S/C16H12F3N3S/c17-16(18,19)14-4-2-1-3-12(14)13(9-20)15(22)23-11-7-5-10(21)6-8-11/h1-8H,21-22H2/b15-13+,
InChiKey:JLOXTZFYJNCPIS-FYWRMAATSA-N,
IUPAC Name:(Z)-3-amino-3-(4-aminophenyl)sulfanyl-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-+4°C, Appropriate long-term storage conditions-+4°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
MEK2 or MAP2K2 is a protein kinase with a mass of approximately 44 kDa. This kinase part of the Mitogen-Activated Protein Kinase (MAPK) pathway primarily functions mechanically as a dual-specificity protein kinase. It phosphorylates both serine/threonine and tyrosine residues on its substrate proteins. MEK2 is largely expressed in various tissues including the brain and heart. It serves an important role in relaying extracellular signals within cells leading to diverse cellular responses.
Biological function summary
MEK2 participates in signal transduction pathways mediating cell division differentiation and apoptosis. As a part of the MAPK signaling cascade it operates downstream of RAS and RAF proteins. MEK2 forms a complex with MEK1 another closely related kinase to ensure proper signal relay. This complex plays a significant role in the regulation of cellular responses to growth signals and stress.
Pathways
MEK2 is intricately connected to the ERK1/2 pathway one of the key pathways it is involved in. ERK1/2 (Extracellular signal-Regulated Kinases) further transmits signals to the cell's nuclear components regulating gene expression critically. MEK2 directly phosphorylates and activates ERK1 and ERK2 facilitating their role in transcription cell cycle regulation and maintenance of cell integrity. The interaction of MEK2 with proteins like BRAF and CRAF along the MAPK pathway amplifies the signal transduction for various growth factors and hormones.
MEK2 has a notable association with cancer particularly melanoma and colorectal cancer. It often becomes aberrantly activated leading to unregulated cell proliferation. The connection of MEK2 to ERK1/2 proteins in these malignancies makes it a potential therapeutic target. Furthermore MEK2 mutations can contribute to Noonan syndrome a disorder that affects multiple body systems marking its relationship with genetic abnormalities and developmental issues. Researchers have been investigating MEK inhibitors to target these disorders highlighting the importance of understanding MEK2's role in disease contexts.
