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454870

39621

≥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
Quality level:
100
Storage condition:
OK to freeze, protect from light
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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 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

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

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

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Anastasia Mashukova et al.
Molecular biology of the cell, 32(8), 690-702 (2021-02-18)
Par1b/MARK2 is a Ser/Thr kinase with pleiotropic effects that participates in the generation of apico-basal polarity in Caenorhabditis elegans. It is phosphorylated by atypical PKC(ι/λ) in Thr595 and inhibited. Because previous work showed a decrease in atypical protein kinase C
Zarin Tabassum et al.
The Journal of biological chemistry, 298(6), 101977-101977 (2022-04-27)
The posttranslational regulation of the neuronal proteome is critical for brain homeostasis but becomes dysregulated in the aged or diseased brain, in which abnormal posttranslational modifications (PTMs) are frequently observed. While the full extent of modified substrates that comprise the

Global Trade Item Number

SKUGTIN
454870-10MG04055977204261