CCG273441
Based on 3 publication(s) in Google Scholar
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 2750414-35-6
- Formula: C26H24ClFN4O3
- Molecular Weight:494.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) CCG273441
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Biological Activity
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GRK2 |
Human GRKs (GRK1 GRK7) are classified into three subfamilies: GRK1 (GRK1 and GRK7), GRK2 (GRK2 and GRK3), and GRK4 (GRK4, GRK5, and GRK6)[1].
CCG273441 (compound 9j) shows moderate potency (GRK5 IC50=3.8 nM) but 1000-fold selectivity over GRK2 (IC50=4.8 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2750414-35-6
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Appearance Solid
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Molecular Weight 494.95
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Formula C26H24ClFN4O3
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Color Yellow to orange
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SMILES
O=C(/C(C1=C2)=C\C3=C(C(NC(CCl)=O)=C(N3)C)C)NC1=CC=C2C(N[C@@H](C4=CC=C(C=C4)F)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Commun Biol
Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]2026 Jan 16;9(1):287. PMID: 41545717 -
iScience
Global functional genomics reveals GRK5 as a cystic fibrosis therapeutic target synergistic with current modulators. [Abstract]2025 Feb 1;28(3):111942. PMID: 40040803 -
Solvent & Solubility
DMSO : 50 mg/mL (101.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0204 mL | 10.1020 mL | 20.2041 mL | 50.5102 mL |
| 5 mM | 0.4041 mL | 2.0204 mL | 4.0408 mL | 10.1020 mL | |
| 10 mM | 0.2020 mL | 1.0102 mL | 2.0204 mL | 5.0510 mL | |
| 15 mM | 0.1347 mL | 0.6735 mL | 1.3469 mL | 3.3673 mL | |
| 20 mM | 0.1010 mL | 0.5051 mL | 1.0102 mL | 2.5255 mL | |
| 25 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0204 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6735 mL | 1.6837 mL | |
| 40 mM | 0.0505 mL | 0.2526 mL | 0.5051 mL | 1.2628 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4041 mL | 1.0102 mL | |
| 60 mM | 0.0337 mL | 0.1684 mL | 0.3367 mL | 0.8418 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2526 mL | 0.6314 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5051 mL |