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CCG 50014

现货
Catalog No.
B2085
RGS4抑制剂
组合的产品项目
规格价格库存 数量
50mg
¥ 3,990.00
Ship with 10-15 days
10mg
¥ 1,030.00
Ship with 10-15 days

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Background

CCG-50014 is a potent and small molecule RGS inhibitor (IC50= 30 nM for RGS4, more than 20 fold selectivity for RGS4 over other RGS proteins). It is a GTPase activating protein that binds to the Gα –subunits of activated heterotrimeric G-proteins and boost GTP hydrolysis rate. [1][2]

RGS (regulator of G protein signaling) inactivates G proteins by promoting GTPase hydrolysis ability of the alphas subunit, thus inhibits the G protein signaling transduction.

In living HEK293T cells, CCG-50014 inhibited Gαo-dependent membrane translocation of GFP-RGS4. HEK293T cell transfected with GFP-RGS4 and Gαo with vehicle (0.1% DMSO) did not changed the membrane localization of RGS4, CCG-50014 (100 μM) reversed the membrane localization of RGS. [1]

References:
[1] Blazer LL, Zhang H, Casey EM et al.  A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry. 2011 Apr 19;50(15):3181-92.
[2] Vashisth H, Storaska AJ, Neubig RR et al.  Conformational dynamics of a regulator of G-protein signaling protein reveals a mechanism of allosteric inhibition by a small molecule. ACS Chem Biol. 2013 Dec 20;8(12):2778-84.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt316.35
Cas No.883050-24-6
FormulaC16H13FN2O2S
SolubilitySoluble in DMSO
Chemical Name4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
SDFDownload SDF
Canonical SMILESCC1=CC=C(C=C1)N2C(=O)N(C(=O)S2)CC3=CC=C(C=C3)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

CCG 50014