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Submit ReviewGRK2i 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.
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.
Solubility | Soluble to 2 mg/ml in water |
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
If you know of a relevant reference for GRK2i, please let us know.
Keywords: GRK2i, GRK2i supplier, GRK, inhibitory, polypeptide, Gbg, antagonists, Gβγ, Gbetagamma, G, protein, heterotrimeric, Heterotrimeric, G-protein, GTPases, 3594, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for GRK2i include:
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
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
Do you know of a great paper that uses GRK2i from Tocris? Please let us know.
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