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Potent and selective GRK2/3 and GRK5/6 inhibitors

Compound 8h and Compound 18 or Compound 19 are highly potent and selective inhibitors of GRK2/3 and GRK5/6, respectively. These compounds are well-tolerated in cellular assays and can be considered the gold standard for GRK inhibitors to date. Using these chemical inhibitors produces results similar to those obtained using GRK knockout (KO) cells in phosphorylation and internalization studies. Therefore, Compound 8h (GRK2/3), Compound 18 (GRK5/6), and their combination can be considered an independent, confirmatory approach to evaluating the GRK specificity of agonist-driven GPCR phosphorylation. Moreover, these chemical inhibitors are ideal for elucidating GRK-specific functions in the regulation of endogenous GPCRs in systems where GRK KO is unavailable.

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Chemical Structure of GRK2/3 Inhibitor (Cmpd 8h) and GRK5/6 Inhibitor (Cmpd 19
GRK Inhibitor Combo Pack 2
5 mg GRK2/3 Inhibitor (Cmpd 8h) + 5 mg GRK5/6 Inhibitor (Cmpd 19) Combo Pack
450.00 € *
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Comparison of GRK5 inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK5/6 Inhibitor (Cmpd 18) or GRK5/6 Inhibitor 2 (Cmpd 19
GRK5/6 Inhibitor 2 (Cmpd 19)
Compound 19 is a potent and selective inhibitor for GRK5 and GRK6. Compound 19 is more potent then Compound 18. CAS No.: 2677786-62-6 Molecular Weight: 423.91 Amount: 5 mg
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Inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK5/6 Inhibitor (Cmpd 18)
GRK5/6 Inhibitor (Cmpd 18)
Compound 18 is a potent and selective inhibitor for GRK5 and GRK6. CAS No.: 2677786-61-5 Molecular Weight: 438.91 Amount: 5 mg
150.00 € *
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Chemical Structure of GRK2/3 Inhibitor (Cmpd 8h) and GRK5/6 Inhibitor (Cmpd 18)
GRK Inhibitor Combo Pack
5 mg GRK2/3 Inhibitor (Cmpd 8h) + 5 mg GRK5/6 Inhibitor (Cmpd 18) Combo Pack
350.00 € *
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Inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK2/3 Inhibitor (Cmpd 8h)
GRK2/3 Inhibitor (Cmpd 8h)
Compound 8h is a potent and selective inhibitor of GRK2 and GRK3. CAS No.: 2592436-21-8 Molecular Weight: 332.36 Amount: 5 mg Solubility: 1 mg/ml in DMSO or Methanol Storage: - 20°C, Protected from light
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Effects of GRK inhibition on phosphorylation of various GPCRs. HEK293 cells stably expressing the β2-adrenergic receptor (β2), the µ-opioid receptor (MOP), the sphingosine-1-phosphate receptor 1 (S1P1),  were were pretreated for 30 min with 30 µM GRK2/3 inhibitor Compound 8h, 30 µM GRK5/6 inhibitor Compound 18, as well as a combination of both compounds or vehicle (V). Cells were then either exposed to 10 µM isoproterenol (ISO), 10 µM (DAMGO), 10 µM fingolimod (FTY) or not exposed. Receptor phosphorylation was analyzed using phosphosite-specific antibodies in a Western blot analysis. Total receptor levels were verified using anti-HA antibodies.

Effects of GRK inhibition on internalization of various GPCRs. HEK293 cells stably expressing the β2-adrenergic receptor (β2), the µ-opioid receptor (MOP), the sphingosine-1-phosphate receptor 1 (S1P1),  were were pretreated for 30 min with 30 µM GRK2/3 inhibitor Compound 8h, 30 µM GRK5/6 inhibitor Compound 18, as well as a combination of both compounds or vehicle (V). Cells were then either exposed to 10 µM isoproterenol (ISO), 10 µM (DAMGO), 10 µM fingolimod (FTY) or not exposed. receptor localization was examined using an anti-HA antibody.

Effects of GRK inhibition on phosphorylation of various GPCRs . HEK293 cells stably expressing the β2-adrenergic receptor (β2), the µ-opioid receptor (MOP), the sphingosine-1-phosphate receptor... read more »
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Potent and selective GRK2/3 and GRK5/6 inhibitors

Effects of GRK inhibition on phosphorylation of various GPCRs. HEK293 cells stably expressing the β2-adrenergic receptor (β2), the µ-opioid receptor (MOP), the sphingosine-1-phosphate receptor 1 (S1P1),  were were pretreated for 30 min with 30 µM GRK2/3 inhibitor Compound 8h, 30 µM GRK5/6 inhibitor Compound 18, as well as a combination of both compounds or vehicle (V). Cells were then either exposed to 10 µM isoproterenol (ISO), 10 µM (DAMGO), 10 µM fingolimod (FTY) or not exposed. Receptor phosphorylation was analyzed using phosphosite-specific antibodies in a Western blot analysis. Total receptor levels were verified using anti-HA antibodies.

Effects of GRK inhibition on internalization of various GPCRs. HEK293 cells stably expressing the β2-adrenergic receptor (β2), the µ-opioid receptor (MOP), the sphingosine-1-phosphate receptor 1 (S1P1),  were were pretreated for 30 min with 30 µM GRK2/3 inhibitor Compound 8h, 30 µM GRK5/6 inhibitor Compound 18, as well as a combination of both compounds or vehicle (V). Cells were then either exposed to 10 µM isoproterenol (ISO), 10 µM (DAMGO), 10 µM fingolimod (FTY) or not exposed. receptor localization was examined using an anti-HA antibody.

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