L 2-401
- Product Name
- L 2-401
- CAS No.
- 883050-24-6
- Chemical Name
- L 2-401
- Synonyms
- CS-563;L 2-401;CCG 50014;CCG50014;CCG 50014;CCG-50014 >=98% (HPLC);CCG-50014, 10 mM in DMSO;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)-;Regulators of G-protein Signaling,Regulator of G-protein Signaling,RGS Protein,CCG-50014,inhibit,CCG50014,Inhibitor
- CBNumber
- CB82657938
- Molecular Formula
- C16H13FN2O2S
- Formula Weight
- 316.35
- MOL File
- 883050-24-6.mol
L 2-401 Property
- 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
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0908
- Product name
- CCG-50014
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $106
- Updated
- 2025/07/31
- Product number
- SML0908
- Product name
- CCG-50014
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $284
- Updated
- 2025/07/31
- Product number
- 10802
- Product name
- CCG-50014
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $27
- Updated
- 2024/03/01
- Product number
- 10802
- Product name
- CCG-50014
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 10802
- Product name
- CCG-50014
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $146
- Updated
- 2024/03/01
L 2-401 Chemical Properties,Usage,Production
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
L 2-401 Preparation Products And Raw materials
Raw materials
Preparation Products
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