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.

• Synonym(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
• Empirical Formula (Hill Notation): C₂₁H₂₁N₃O₃S
• CAS Number: 895112-95-5
• Molecular Weight: 395.47
• MDL number: MFCD07656268
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 100 mg/mL, clear, yellow
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O=C1C(SCC(NC2=C(C)C=CC(C)=C2)=O)=NC=CN1C3=CC=C(C=C3)OC

Description

General description

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).

A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK-selective inhibitor (IC₅₀ = 3.6 µM; [ATP] = 100 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 in CHO cells (10 µM).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable