554995-M
RGS Proteins Inhibitor II, CCG-50014
The RGS Proteins Inhibitor II, CCG-50014 controls the biological activity of RGS4 proteins. This small molecule/inhibitor is primarily used for Biochemicals applications.
Synonym(s):
RGS Proteins Inhibitor II, CCG-50014, 4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
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About This Item
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Quality Level
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
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).
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).
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Blazer, L.L., et al. 2011. Biochemistry50, 3181.
Roman, D.L., et al. 2009. J. Biomol. Screening14, 610.
Roman, D.L., et al. 2009. J. Biomol. Screening14, 610.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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