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454870

39621

Name: 39621
Brand: MM

≥98% (HPLC), ATP-competitive MARK inhibitor, solid

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

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About This Item

Empirical Formula (Hill Notation):

C₂₁H₂₁N₃O₃S

CAS Number:

895112-95-5

Molecular Weight:

395.47

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD07656268

Assay:

≥98% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

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.

Quality Segment

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

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)

InChI key

CGRJEWQUCBVSJR-UHFFFAOYSA-N

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).

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c