For research use only. Not for therapeutic Use.
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site[1]. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test[2].
CCG50014 (10, 30, or 100 nM) attenuates the nociceptive responses during the late phase in a dose-dependent manner[2].
Catalog Number | I005892 |
CAS Number | 883050-24-6 |
Synonyms | 4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione |
Molecular Formula | C16H13FN2O2S |
Purity | ≥95% |
InChI | InChI=1S/C16H13FN2O2S/c1-11-2-8-14(9-3-11)19-15(20)18(16(21)22-19)10-12-4-6-13(17)7-5-12/h2-9H,10H2,1H3 |
InChIKey | QUIIIYITNGOFEI-UHFFFAOYSA-N |
SMILES | CC1=CC=C(C=C1)N2C(=O)N(C(=O)S2)CC3=CC=C(C=C3)F |
Reference | [1]. Blazer LL, et al. A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry. 2011 Apr 19;50(15):3181-92. [2]. Yoon SY, et al. Intrathecal RGS4 inhibitor, CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test. Anesth Analg. 2015 Mar;120(3):671-7. |