| Bioactivity | CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2]. |
| Target | CRTh2EC50: 2 μM (PDK1)Ki: 8.4 μM (PDK1) |
| Invitro | CRTh2 antagonist 3 (compound 4) is a small-molecule allosteric modulator of the protein kinase PDK1 from structure-based docking. CRTh2 antagonist 3 is 5-fold more potent than its parent compound[2]. |
| Name | CRTh2 antagonist 3 |
| CAS | 312928-72-6 |
| Formula | C19H20N2O3S |
| Molar Mass | 356.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
CRTh2 antagonist 3
CAS: 312928-72-6 F: C19H20N2O3S W: 356.44
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. C
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