CCG-50014

SKU: orb1300770

Description

CCG-50014 is a highly potent and selective small molecule inhibitor of Regulator of G-protein Signaling 4 (RGS4), exhibiting an IC50 value of 30 nM. This compound is a valuable research tool for investigating RGS4 function in both cellular and animal models of neurological disorders, including Parkinson's disease and schizophrenia.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 883050-24-6
• MW: 316.35
• Purity: 98.69% (May vary between batches)
• Formula: C₁₆H₁₃FN₂O₂S
• SMILES: Cc1ccc(cc1)-n1sc(=O)n(Cc2ccc(F)cc2)c1=O
• Target: GTPase
• Solubility: DMSO:59 mg/mL (186.5 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  RGS4:30 nM|RGS16:3.5 μM|RGS8:11 μM|RGS19:0.12 μM
• In Vitro:
  CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys ). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4 Gαo protein protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment.
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Storage & Handling

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

Alternative Names

CCG 50014, CCG50014, CCG-50014, Inhibitor, inhibit, Regulator of G-protein Signaling, RGS4, RGS8, RGS Protein, RGS16, RGS19, Regulators of G-protein Signaling

Compound Identifiers

PubChem CID

2733079