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

Properties

• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable