| Identification | Back Directory | [Name]
L 2-401 | [CAS]
883050-24-6 | [Synonyms]
CS-563
L 2-401
CCG 50014
CCG50014;CCG 50014
CCG-50014 >=98% (HPLC)
4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
4-[(4-Fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
1,2,4-Thiadiazolidine-3,5-dione, 4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C16H13FN2O2S | [MDL Number]
MFCD00113783 | [MOL File]
883050-24-6.mol | [Molecular Weight]
316.35 |
| Chemical Properties | Back Directory | [density ]
1.398±0.06 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear (warmed) | [form ]
powder | [color ]
white to beige | [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]
Fc1ccc(cc1)C[n]2[c]([s][n]([c]2=O)c3ccc(cc3)C)=O |
| Hazard Information | Back Directory | [Description]
CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins. RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins. CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane. | [Uses]
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]. | [in vivo]
CCG50014 (10, 30, or 100 nM) attenuates the nociceptive responses during the late phase in a dose-dependent manner[2]. | [IC 50]
RGS4: 30 nM (IC50); RGS8: 11 μM (IC50); RGS16: 3.5 μM (IC50); RGS19: 0.12 μM (IC50) | [References]
[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. DOI:10.1021/bi1019622
[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. DOI:10.1213/ANE.0000000000000607 |
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