454870

MARK/Par-1 Activity Inhibitor, 39621

The MARK/Par-1 Activity Inhibitor, 39621 controls the biological activity of MARK/Par-1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): MARK/Par-1 Activity Inhibitor, 39621, Microtubule Affinity Regulating Kinase Inhibitor, MAP Affinity Regulating Kinase Inhibitor, PAR1 Inhibitor, N-(2,5-Dimethylphenyl)-2-(4-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrazin-2-ylthio)acetamide, N-(2,5-Dimethylphenyl)-2-(4-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrazin-2-ylthio)acetamide, Microtubule Affinity Regulating Kinase Inhibitor, MAP Affinity Regulating Kinase Inhibitor, PAR1 Inhibitor
• Fórmula empírica (Notação de Hill): C₂₁H₂₁N₃O₃S
• Número CAS: 895112-95-5
• Peso molecular: 395.47
• Número MDL: MFCD07656268
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: beige
• solubilidade: DMSO: 100 mg/mL, clear, yellow
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: O=C1C(SCC(NC2=C(C)C=CC(C)=C2)=O)=NC=CN1C3=CC=C(C=C3)OC
• InChI: 1S/C21H21N3O3S/c1-14-4-5-15(2)18(12-14)23-19(25)13-28-20-21(26)24(11-10-22-20)16-6-8-17(27-3)9-7-16/h4-12H,13H2,1-3H3,(H,23,25)
• chave InChI: CGRJEWQUCBVSJR-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK inhibitor (IC₅₀ = 3.6 µM; [ATP] = 100 µM) with much reduced or little activity against GSK-3β, SAD-kinase B/BRSK-1, MARKK/TAO-1, Cdc2/cycB, and p38/SAPK (30%, 20%, 11%, 4%, and 0% inhibition, respectively; [inhibitor] = 50 µM). Shown to effectively block primary rat cortical neuron axon growth (5.7 µm/hr vs 32.5 µm/hr with or without 20 µM inhibitor) and prevent MARK2 overexpression-induced Tau Ser262 phosphorylation and cytotoxicity due to microtubule network breakdown in CHO cells (10 µM).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Timm, T., et al. 2011. J. Biol. Chem.286, 41711.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable