CCG-215022

SKU: orb1225879

Description

CCG-215022 (CCG215022) is a potent and selective pan GRK (G protein-coupled receptor kinase) inhibitor with IC50 of 0.15/0.38/3.9 uM for GRK2/5/1 respectively; displays 300-800 fold selectivity against PKA; exhibits improved potency compared with GSK180736A.

Key Properties

• CAS Number: 1813527-81-9
• MW: 499.4964
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₂FN₇O₃
• SMILES: O=C(C1=C(F)C=CC(C2C(C(NC3=CC=C(NN=C4)C4=C3)=O)=C(C)NC(N2)=O)=C1)NCC5=NC=CC=C5
• Target: GRK (GPCRK)
• Solubility: DMSO: ≥ 28 mg/mL

Bioactivity

• In Vitro:
  CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCG215022 | CCG 215022

Quick Database Links

Gene Symbol

GRK (GPCRK)