|CCG 50014游离态|CsnPharm

CAS No.: 883050-24-6

CCG-50014 Catalog No. CSN16484

Synonyms: Ccg 50014

CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.

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描述The regulator of G-protein signaling (RGS) proteins are negative regulators of the G-protein coupled receptors signaling pathways. CCG 50014 is a potent, irreversible small molecule inhibitor of RGS4 with an IC50 value of 30nM. It also inhibits other RGS proteins, including RGS8, 16, and 19 with IC50 values of 11, 3.5, and 0.12μM, respectively. CCG 50014 at 10μM inhibited the GTPase accelerating activity of RGS4 and RGS8 on Gα₀. Compared to vehicle-treated protein, wild-type RGS8 treated with 100μM CCG 50014 was 14-fold less potent at competing for Gα binding. When treated with CCG 50014 at 20μM, the binding of 107C RGS8 to Gα was inhibited by ~20% and the binding of 160C RGS8 to Gα was inhibited by ~50%. CCG 50014 at 100μM inhibited Gα₀-dependent membrane translocation of GFP-RGS4 in living HEK293T cells.^[3] The intrathecal administration with CCG50014 (10, 30, or 100nmol) dose-dependently attenuated nociceptive responses and enhanced opioid-mediated analgesic effects in mice injected with formalin.^[4]
作用机制CCG 50014 may inhibit RGS protein through sulfhydryl modification. It covalently binds to RGS protein, forming an adduct on two cysteine residues located in an allosteric regulatory site.^[3]
参考文献

[1] Turner EM, Blazer LL, et al. Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins. ACS Med Chem Lett. 2012 Feb 9;3(2):146-150.
[2] Blazer LL, Zhang H, et al. A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry. 2011 Apr 19;50(15):3181-92.
[3] Blazer LL, Zhang H, Casey EM, Husbands SM, Neubig RR. A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry.2011;50(15):3181‐3192. doi:10.1021/bi1019622
[4] Yoon SY, Woo J, Park JO, et al. Intrathecal RGS4 inhibitor, CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test. Anesth Analg. 2015;120(3):671‐677. doi:10.1213/ANE.0000000000000607

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1611 mL
- 15.8053 mL
- 31.6106 mL
- 5 mM
- 0.6322 mL
- 3.1611 mL
- 6.3221 mL
- 10 mM
- 0.3161 mL
- 1.5805 mL
- 3.1611 mL

技术信息

CAS号

883050-24-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H13FN2O2S

运输

蓝冰

分子量

316.35

别名

Ccg 50014

溶解度

DMSO	63.0 mg/mL (199.1 mM)
Water	Insoluble
Ethanol	Insoluble

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