1. GPCR/G Protein
  2. G Protein-coupled Receptor Kinase (GRK)
  3. CCG273441

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.

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CCG273441 Chemical Structure

CCG273441 Chemical Structure

CAS No. : 2750414-35-6

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5 mg USD 265 In-stock
10 mg USD 420 In-stock
25 mg USD 850 In-stock
50 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

IC50: 3.8 nM (human GRK5), 19 nM (GRK5-C474S), 4.8 μM (bovine GRK2)[1]

In Vitro

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.

Molecular Weight

494.95

Formula

C26H24ClFN4O3

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0204 mL 10.1020 mL 20.2041 mL
5 mM 0.4041 mL 2.0204 mL 4.0408 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.67%

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
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CCG273441 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CCG273441
Cat. No.:
HY-47573
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