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CRTh2 antagonist 3

Catalog No. T10890   CAS 312928-72-6

CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the potential to cause cardiovascular inflammation.

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CRTh2 antagonist 3 Chemical Structure
CRTh2 antagonist 3, CAS 312928-72-6
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the potential to cause cardiovascular inflammation.
Targets&IC50 PDK1:2 μM (EC50), PDK1:8.4 μM (Ki)
In vitro CRTh2 antagonist 3 is a small molecule allosteric modulator of structure-based docking protein kinase PDK1. CRTh2 antagonist 3 is 5 times more potent than its parent compound.
Molecular Weight 356.44
Formula C19H20N2O3S
CAS No. 312928-72-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Heinz Fretz, et al. 2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists. US8273740B2. 2. Rettenmaier TJ, et al. Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking. J Med Chem. 2015 Oct 22;58(20):8285-8291.

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Keywords

CRTh2 antagonist 3 312928-72-6 Others CRTh-2 antagonist 3 inhibitor inhibit

 

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