2. GPCR/G Protein
  3. G Protein-coupled Receptor Kinase (GRK)
  4. GRK2 degrader-1

GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research.

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GRK2 degrader-1

GRK2 degrader-1 Chemical Structure

CAS No. : 3052947-04-0

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GRK2 degrader-1 Related Antibodies

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Description

GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research[1].

IC50 & Target[1]

GRK2

 

Molecular Weight

474.53

Formula

C25H22N4O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CC1=CC=C2C(C(N(C3C(NC(CC3)=O)=O)C2)=O)=C1)NC4=NC=C(CC5=CC=CC=C5)S4
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 : 100 mg/mL (210.73 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 2.1073 mL 10.5367 mL 21.0735 mL
5 mM 0.4215 mL 2.1073 mL 4.2147 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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
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 2.1073 mL 10.5367 mL 21.0735 mL 52.6837 mL
5 mM 0.4215 mL 2.1073 mL 4.2147 mL 10.5367 mL
10 mM 0.2107 mL 1.0537 mL 2.1073 mL 5.2684 mL
15 mM 0.1405 mL 0.7024 mL 1.4049 mL 3.5122 mL
20 mM 0.1054 mL 0.5268 mL 1.0537 mL 2.6342 mL
25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7561 mL
40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3171 mL
50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8781 mL
80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
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GRK2 degrader-1 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.

Keywords:

GRK2 degrader-13052947-04-0G Protein-coupled Receptor Kinase (GRK)ubiquitin-proteasome pathwayGRK2pulmonary artery hypertensionInhibitorinhibitorinhibit

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