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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.78%
- CAS 番号: 2750414-35-6
- 分子式: C26H24ClFN4O3
- 分子量:494.95
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 CCG273441
More
生物活性
|
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.
化学情報
-
CAS 番号 2750414-35-6
-
性状 Solid
-
分子量 494.95
-
分子式 C26H24ClFN4O3
-
Color Yellow to orange
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
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 -
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (272 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
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 |