CCG-50014
Based on 2 publication(s) in Google Scholar
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. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
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- Pureza : 99.62%
- No. CAS: 883050-24-6
- Fòrmula: C16H13FN2O2S
- Peso molecular:316.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CCG-50014
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
RGS4 30 nM (IC50) |
RGS8 11 μM (IC50) |
RGS16 3.5 μM (IC50) |
RGS19 0.12 μM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 883050-24-6
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Appearance Solid
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Peso molecular 316.35
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Fòrmula C16H13FN2O2S
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Color White to light yellow
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SMILES
O=C(N1CC2=CC=C(F)C=C2)N(C3=CC=C(C)C=C3)SC1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Neurotherapeutics
The Antipsychotic Drug Clozapine Suppresses the RGS4 Polyubiquitylation and Proteasomal Degradation Mediated by the Arg/N-Degron Pathway. [Abstract]2021 Jul;18(3):1768-1782. PMID: 33884581 -
J Biol Chem
MGST3 regulates BACE1 protein translation and amyloidogenesis by controlling the RGS4-mediated AKT signaling pathway. [Abstract]2024 Aug;300(8):107530. PMID: 38971310
Solvente y solubilidad
In Vitro:
DMSO : 62.5 mg/mL (197.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1611 mL | 15.8053 mL | 31.6106 mL | 79.0264 mL |
| 5 mM | 0.6322 mL | 3.1611 mL | 6.3221 mL | 15.8053 mL | |
| 10 mM | 0.3161 mL | 1.5805 mL | 3.1611 mL | 7.9026 mL | |
| 15 mM | 0.2107 mL | 1.0537 mL | 2.1074 mL | 5.2684 mL | |
| 20 mM | 0.1581 mL | 0.7903 mL | 1.5805 mL | 3.9513 mL | |
| 25 mM | 0.1264 mL | 0.6322 mL | 1.2644 mL | 3.1611 mL | |
| 30 mM | 0.1054 mL | 0.5268 mL | 1.0537 mL | 2.6342 mL | |
| 40 mM | 0.0790 mL | 0.3951 mL | 0.7903 mL | 1.9757 mL | |
| 50 mM | 0.0632 mL | 0.3161 mL | 0.6322 mL | 1.5805 mL | |
| 60 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3171 mL | |
| 80 mM | 0.0395 mL | 0.1976 mL | 0.3951 mL | 0.9878 mL | |
| 100 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7903 mL |
CCG-50014 Related Classifications
HY-13509 Related Classifications
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