Home GPCR & G Protein RGS inhibitor CCG 50014

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CCG 50014 RGS inhibitor

Cat.No.S2901

CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.
CCG 50014 RGS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 316.35

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S290101 DMSO]63 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.91%
99.91

Chemical Information, Storage & Stability

Molecular Weight 316.35 Formula

C16H13FN2O2S

 Storage (From the date of receipt)
CAS No. 883050-24-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)N2C(=O)N(C(=O)S2)CC3=CC=C(C=C3)F

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (199.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
RGS4 [1]
30 nM
RGS19 [1]
0.12 μM
RGS16 [1]
3.5 μM
RGS8 [1]
11 μM
In vitro
CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys−). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4−Gαo protein−protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment. [1] [2]
References

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