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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[1].

Product Specifications

CAS Number

[3052947-04-0]

UNSPSC

12352005

Target

G Protein-coupled Receptor Kinase (GRK)

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

O=C(CC1=CC=C2C(C(N(C3C(NC(CC3)=O)=O)C2)=O)=C1)NC4=NC=C(CC5=CC=CC=C5)S4

Molecular Formula

C25H22N4O4S

Molecular Weight

474.53

References & Citations

[1]Zuling XU, et al. G protein-coupled receptor kinase 2 (grk2) degradation compounds and use thereof. WO2024165075. 2024-08-15

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

GRK2

Curated Selection

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