MK-2 Inhibitor IIIA cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor

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MK-2 Inhibitor III (CAS 1186648-22-5)

MK-2 Inhibitor III | CAS 1186648-22-5 is rated 5.0 out of 5 by 1.

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Synonym: 2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one

Application: A cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor

CAS Number: 1186648-22-5

Purity: ≥97%

Molecular Weight: 358.39

Molecular Formula: C₂₁H₁₆N₄O•H₂O

* Refer to Certificate of Analysis for lot specific data (including water content).

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• Description
• Technical Information
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• SDS & Certificate of Analysis

MK-2 Inhibitor III is a cell-permeable pyrrolopyridinyl compound that acts as a potent, selective, and ATP-biniding site-targeting MK-2/MAPKAP-K2 inhibitor (IC₅₀ = 8.5, 81, and 210 nM agaisnt MAPKAPK-2 (MK-2), PRAK(MK-5), and 3pK(MK-3), respectively), while exhibiting much less or no activity against 8 other commonly studied kinases. Shown to suppress LPS-induced TNF-α production in U937 cells (IC₅₀ = 4.4 μM).

References

Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647.

Physical State :

Solid

Solubility :

Soluble in DMSO (50 mg/ml).

Storage :

Store at 4° C

Boiling Point :

784.9° C at 760 mmHg (Predicted)

Refractive Index :

n²⁰_D 1.70 (Predicted)

IC50 :

MAPKAPK-2 : IC₅₀ = 8.5 nM; PRAK: IC₅₀ = 81 nM; 3pK: IC₅₀ = 210 nM; LPS-induced TNF-α production: IC₅₀ = 4.4 µM (U937 cells)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

25163932

SMILES :

C1CNC(=O)C2=C1NC(=C2)C3=CC(=NC=C3)C4=CC5=CC=CC=C5N=C4.O

Download SDS (MSDS)

Region US - English Brazil - Portuguese Canada - English Canada - French China - Chinese Europe - English Europe - French Europe - German Europe - Italian Europe - Spanish Korea - Korean Japan - Japanese Mexico - Spanish

Certificate of Analysis

Catalog Number sc-221948

Lot Number

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MK-2 Inhibitor III  Product Citations

See how others have used MK-2 Inhibitor III. Click on the entry to view the PubMed entry .

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PMID: # 26505478  Matsuzaki, H. et al. 2015. PLoS ONE. 10: e0141746.

PMID: # 23657501  Mao, X. et al. 2014. J. Invest. Dermatol. 134: 68-76.

Citations 1 to 2 of 2 total

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Rated 5 out of 5 by MS from Soukup et al Soukup et al. (PubMed ID 26078274) found that MK-2 Inhibitor III inactivated MK2-mediated p38 inhibition and enabled dendritic cells to strengthen proinflammatory mechanisms by potentiating IL-1 -mediated Th1 activity in mice with encephalomyelitis. -SCBT Publication Review

Date published: 2015-05-02

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