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CCG-50014

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Chemical Structure| 883050-24-6 同义名 : -
CAS号 : 883050-24-6
货号 : A264294
分子式 : C16H13FN2O2S
纯度 : 99%+
分子量 : 316.35
MDL号 : MFCD00113783
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(189.66 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.81mL

3.16mL

1.58mL

31.61mL

6.32mL

3.16mL
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