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Submit ReviewGRK2i
Discontinued Product
3594 has been discontinued.
View all Heterotrimeric G-protein GTPases products.
Description: GRK2 inhibitory polypeptide; Gβ/γ antagonist
Purity: ≥95% (HPLC)
Biological Activity for GRK2i
GRK2i is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. Corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.
Technical Data for GRK2i
| M. Wt | 3484.08 |
| Formula | C153H256N50O41S |
| Sequence | WKKELRDAYREAQQLVQRVPKMKNKPRS |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 148505-03-7 |
| PubChem ID | 90488863 |
| InChI Key | QYWJBYYWQATYFS-ICUWLHSYSA-N |
| Smiles | [H]N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for GRK2i
References for GRK2i
References are publications that support the biological activity of the product.
Koch et al (1994) Cellular expression of the carboxyl terminus of a G protein-coupled receptor kinase attenuates Gβγ-mediated signaling. J.Biol.Chem. 269 6193 PMID: 8119963
Macrez et al (1997) A βγ dimer derived from G13 transduces the angiotensin AT1 receptor signal to stimulation of Ca2+ channels in rat portal vein myocytes. J.Biol.Chem. 272 23180 PMID: 9287322
Dang et al (2009) Two distinct mechanisms mediate acute μ-opioid receptor desensitization in native neurons. J.Neurosci. 29 3322 PMID: 19279269
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Keywords: GRK2i, GRK2i supplier, GRK, inhibitory, polypeptide, Gbg, antagonists, Gβγ, Gbetagamma, G, protein, heterotrimeric, Heterotrimeric, G-protein, GTPases, 3594, Tocris Bioscience
4 Citations for GRK2i
Citations are publications that use Tocris products. Selected citations for GRK2i include:
Lutz et al (2021) Gαo is a major determinant of cAMP signaling in the pathophysiology of movement disorders. Cell Rep 34 108718 PMID: 33535037
Kirill A et al (2019) Homeostatic cAMP regulation by the RGS7 complex controls depression-related behaviors. Neuropsychopharmacology 44 642-653 PMID: 30546127
Sierra-Fonseca et al (2014) Nerve growth factor induces neurite outgrowth of PC12 cells by promoting Gβγ-microtubule interaction. BMC Neurosci 15 132 PMID: 25552352
Stott et al (2015) G-protein βγ subunits are positive regulators of Kv7.4 and native vascular Kv7 channel activity. Apoptosis 112 6497 PMID: 25941381
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