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AB120082

SL 327, MEK inhibitor

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(7 Publications)

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).
1 Images
Chemical Structure - SL 327, MEK inhibitor (AB120082)
  • Chemical Structure

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Chemical Structure - SL 327, MEK inhibitor (AB120082)

2D chemical structure image of ab120082, SL 327, MEK inhibitor

Key facts

CAS number

305350-87-2

Purity

>99%

Form

Solid

form

Molecular weight

335.3 Da

Molecular formula

C<sub>1</sub><sub>6</sub>H<sub>1</sub><sub>2</sub>F<sub>3</sub>N<sub>3</sub>S

PubChem

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

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.

Product protocols

Publications (7)

Recent publications for all applications. Explore the full list and refine your search

The European journal of neuroscience 34:190-8 PubMed21692887

2011

Brain-derived neurotrophic factor rapidly increases AMPA receptor surface expression in rat nucleus accumbens.

Applications

Unspecified application

Species

Unspecified reactive species

Xuan Li,Marina E Wolf

British journal of pharmacology 163:857-75 PubMed21615389

2011

Protein kinase C phosphorylates the cAMP response element binding protein in the hypothalamic paraventricular nucleus during morphine withdrawal.

Applications

Unspecified application

Species

Unspecified reactive species

F Martín,L Mora,Ml Laorden,Mv Milanés

Brain, behavior, and immunity 25 Suppl 1:S146-54 PubMed21377524

2011

Cytokine involvement in stress may depend on corticotrophin releasing factor to sensitize ethanol withdrawal anxiety.

Applications

Unspecified application

Species

Unspecified reactive species

Darin J Knapp,Buddy A Whitman,Tiffany A Wills,Robert A Angel,David H Overstreet,Hugh E Criswell,Zhen Ming,George R Breese

Behavioural brain research 217:399-407 PubMed21074569

2010

Inhibition of extracellular signal-regulated kinase (ERK) activity with SL327 does not prevent acquisition, expression, and extinction of ethanol-seeking behavior in mice.

Applications

Unspecified application

Species

Unspecified reactive species

Peter A Groblewski,Frederick H Franken,Christopher L Cunningham

Neuropsychopharmacology : official publication of 34:2477-88 PubMed19606087

2009

Differential involvement of D1 and D2 dopamine receptors in L-DOPA-induced angiogenic activity in a rat model of Parkinson's disease.

Applications

Unspecified application

Species

Unspecified reactive species

Hanna S Lindgren,K Elisabet Ohlin,M Angela Cenci

The Journal of pharmacology and experimental thera 330:771-82 PubMed19567779

2009

Cross-talk between protein kinase A and mitogen-activated protein kinases signalling in the adaptive changes observed during morphine withdrawal in the heart.

Applications

Unspecified application

Species

Unspecified reactive species

P Almela,N M Atucha,M V Milanés,M L Laorden

British journal of pharmacology 155:73-83 PubMed18536752

2008

The 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 application

Species

Unspecified reactive species

P Almela,Mv Milanés,Ml Laorden
View all publications

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