[CAS NO. 883050-24-6] CCG 50014

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PRODUCTS SPECIFICATIONS [883050-24-6]

Catalog

SLK-S2901

Brand

Selleck

CAS

883050-24-6

DESCRIPTION [883050-24-6]

Overview

MDL	MFCD00113783
Molecular Weight	316.35
Molecular Formula	C16H13FN2O2S
SMILES	O=C(N1CC2=CC=C(F)C=C2)N(C3=CC=C(C)C=C3)SC1=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.1611 mL	15.8053 mL	31.6106 mL
5 mM	0.6322 mL	3.1611 mL	6.3221 mL
10 mM	0.3161 mL	1.5805 mL	3.1611 mL
50 mM	0.0632 mL	0.3161 mL	0.6322 mL

Description

CCG 50014 is a potent and selective inhibitor of with of 30 nM.

Targets

RGS4 ^[1]	RGS19 ^[1]	RGS16 ^[1]	RGS8 ^[1]
30 nM	0.12 μM	3.5 μM	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.

References

[1] Blazer LL, et al. Biochemistry, 2011, 50(15), 3181-3192.
[2] Turner EM, et al. ACS Med Chem Lett, 2012, 3(2), 146-150.