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554995-M

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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

Empirical Formula (Hill Notation):
C16H13FN2O2S
Molecular Weight:
316.35
UNSPSC Code:
12352202

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.

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)

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