CCG-4986 | RGS4 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $220.00 |
CCG-4986 (7134-19-2) is the first selective non-peptide inhibitor of the regulator of G protein signaling protein subtype RGS4.1 It covalently2-3 modifies RGS4 by inhibiting its interaction with Gα (IC50 = 3-5 mM) and suppressing GTPase activity1. Intratympanic administration of CCG-4986 was shown to rescue cochlear injury and hearing loss induced by acoustic overexposure and represents a novel paradigm for the treatment of sensorineural hearing loss via pharmacological regulation of GPCR signaling.4 A novel tool for exploring the involvement of RGS4 in physiological processes.5
References/Citations:
- Roman et al. (2007), Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay; Mol. Pharmacol. 71 169
- Kimple et al. (2007), The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Galpha-interaction face; Biochim. Biophys. Acta. 1774 1213
- Roman et al. (2010), Allosteric inhibition of the regulator of G protein signaling-Galpha protein-protein interaction by CCG-4986; Mol. Pharmacol. 71 360
- Fok et al. (2020), Regulator of G Protein Signaling 4 (RGS4) as a Novel Target for the Treatment of Sensorineural Hearing Loss; Int. J. Mol. Sci. 22 3
- Cheng et al. (2013), Zebrafish rgs4 is essential for motility and axonogenesis mediated by Akt signaling; Cell. Mol. Life Sci. 70 935
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
CCG-4986 (7134-19-2) is the first selective non-peptide inhibitor of the regulator of G protein signaling protein subtype RGS4.1 It covalently2-3 modifies RGS4 by inhibiting its interaction with Gα (IC50 = 3-5 mM) and suppressing GTPase activity1. Intratympanic administration of CCG-4986 was shown to rescue cochlear injury and hearing loss induced by acoustic overexposure and represents a novel paradigm for the treatment of sensorineural hearing loss via pharmacological regulation of GPCR signaling.4 A novel tool for exploring the involvement of RGS4 in physiological processes.5
References/Citations:
- Roman et al. (2007), Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay; Mol. Pharmacol. 71 169
- Kimple et al. (2007), The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Galpha-interaction face; Biochim. Biophys. Acta. 1774 1213
- Roman et al. (2010), Allosteric inhibition of the regulator of G protein signaling-Galpha protein-protein interaction by CCG-4986; Mol. Pharmacol. 71 360
- Fok et al. (2020), Regulator of G Protein Signaling 4 (RGS4) as a Novel Target for the Treatment of Sensorineural Hearing Loss; Int. J. Mol. Sci. 22 3
- Cheng et al. (2013), Zebrafish rgs4 is essential for motility and axonogenesis mediated by Akt signaling; Cell. Mol. Life Sci. 70 935
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