MW 335.3 Da, Purity >99%. Centrally active, brain penetrant selective MEK1 and MEK2 inhibitor (IC50 values in in vitro assays are 0.18 and 0.22 μM, respectively).
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- The European journal of neuroscience 34:190-82011Brain-derived neurotrophic factor rapidly increases AMPA receptor surface expression in rat nucleus accumbens.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXuan Li et. al.PubMed 21692887
- British journal of pharmacology 163:857-752011Protein kinase C phosphorylates the cAMP response element binding protein in the hypothalamic paraventricular nucleus during morphine withdrawal.Applications:Unspecified applicationReactive species:Unspecified reactive speciesF Martín,L Mora,Ml Laorden,Mv MilanésPubMed 21615389
- Brain, behavior, and immunity 25 Suppl 1:S146-542011Cytokine involvement in stress may depend on corticotrophin releasing factor to sensitize ethanol withdrawal anxiety.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDarin J Knapp et. al.PubMed 21377524
- Behavioural brain research 217:399-4072010Inhibition of extracellular signal-regulated kinase (ERK) activity with SL327 does not prevent acquisition, expression, and extinction of ethanol-seeking behavior in mice.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPeter A Groblewski,Frederick H Franken,Christopher L CunninghamPubMed 21074569
- Neuropsychopharmacology : official publication of 34:2477-882009Differential involvement of D1 and D2 dopamine receptors in L-DOPA-induced angiogenic activity in a rat model of Parkinson's disease.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHanna S Lindgren et. al.PubMed 19606087
- The Journal of pharmacology and experimental thera 330:771-822009Cross-talk between protein kinase A and mitogen-activated protein kinases signalling in the adaptive changes observed during morphine withdrawal in the heart.Applications:Unspecified applicationReactive species:Unspecified reactive speciesP Almela et. al.PubMed 19567779
- British journal of pharmacology 155:73-832008The PKs PKA and ERK 1/2 are involved in phosphorylation of TH at Serine 40 and 31 during morphine withdrawal in rat hearts.Applications:Unspecified applicationReactive species:Unspecified reactive speciesP Almela,Mv Milanés,Ml LaordenPubMed 18536752
Key facts
- CAS number
- 305350-87-2
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 335.3 Da
- Molecular formula
- C16H12F3N3S
- PubChem identifier
- 9549284
- Nature
- Synthetic
Target data
Alternative names
CFC syndrome, CFC4, Cardiofaciocutaneous syndrome, Dual specificity mitogen-activated protein kinase kinase 2, ERK activator kinase 2, FLJ26075, MAP kinase kinase 2, MAP2K2, MAPK / ERK kinase 2, MAPKK 2, MEK 2, MKK 2, MP2K2_HUMAN, Microtubule associated protein kinase kinase 2, Mitogen activated protein kinase kinase 2, Mitogen activated protein kinase kinase 2 p45, OTTHUMP00000165826, OTTHUMP00000165827, PRKMK 2
Recommended products
MW 335.3 Da, Purity >99%. Centrally active, brain penetrant selective MEK1 and MEK2 inhibitor (IC50 values in in vitro assays are 0.18 and 0.22 μM, respectively).
Key facts
- CAS number
- 305350-87-2
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 335.3 Da
- Molecular formula
- C16H12F3N3S
- PubChem identifier
- 9549284
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
Soluble 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
Storage
- 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 info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
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.
- Associated diseases and disorders
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.
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Chemical Structure - SL 327, MEK inhibitor (ab120082)
2D chemical structure image of ab120082, SL 327, MEK inhibitor
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