CCG215022

SKU: orb1304144

Description

CCG215022

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1813527-81-9
• MW: 499.5
• Purity: 97.63%
• Formula: C₂₆H₂₂FN₇O₃
• SMILES: CC1=C(C(NC(=O)N1)c1ccc(F)c(c1)C(=O)NCc1ccccn1)C(=O)Nc1ccc2[nH]ncc2c1
• Target: PKA,GRK
• Solubility: DMSO:50 mg/mL (100.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4 mM)

Bioactivity

• Target IC50:
  GRK2:0.15±0.07 μM|GRK1:3.9±1 μM|GRK5:0.38±0.06 μM
• In Vitro:
  CCG215022 demonstrates nanomolar potency against both GRK2 and GRK5, outperforming Paroxetine by being at least 20-fold more potent. A GRK2 structure-based drug design campaign revealed CCG215022's nanomolar IC50 values against GRK2 and GRK5, alongside significant selectivity over other closely related kinases, including GRK1 and PKA. When applied to murine cardiomyocytes, CCG215022 significantly enhances contractility at concentrations 20-fold lower than those required for Paroxetine, which exhibits modest selectivity for GRK2.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCG-215022, CCG215022, CCG 215022, GRK5, GRK1, GRK2, Inhibitor, inhibit, Protein kinase A, PKA

Compound Identifiers

PubChem CID

118888941