|
RGS Proteins Inhibitor II, CCG-50014
4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
A cell-permeable thiadiazolidinedione compound that acts as a direct, potent, selective and cysteine-reactive irreversible inhibitor of RGS4 over other RGS proteins (IC50 = 0.03, 0.12, 3.5, 11, > 200 and > 200 µM against RGS4, RGS19, RGS16, RGS8, RGS7 and RGS4Cys− using FCPIA assay, respectively). Shown to block RGS4-Gα0 interaction and repress Gα0-dependent membrane localization of RGS4 in HEK-293T cells with no effect on the intrinsic rate of GTP hydrolysis by Gα0. Suggested to interact with Cys107-RGS8 allosteric regulatory site and display minimal affinity towards papain (IC50 > 100 µM). A reversible inhibitor of RGS Proteins, CCG-63802 is also available (Cat. No. 554993).
产品信息
Form White solid
Molar mass 316.4
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C16H13FN2O2S
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |