RHC-80267 - CAS 83654-05-1 - CALBIOCHEM (C005B-474609)

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