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KT 5720 is a specific, reversible, ATP-competitive, cell-permeable protein kinase A (PKA) inhibitor with an IC50 value of 3.3 μM, which effectively reverses MDR1-mediated multidrug resistance and reduces excitability of dorsal root ganglion (DRG) neurons by attenuating the activity of hyperpolarization-activated cyclic nucleotide-gated cation (HCN) channels and decreasing the intracellular Ca2+ concentration. ) neurons by reducing hyperpolarization-activated cyclic nucleotide-gated cation (HCN) channel activity and intracellular Ca2+ concentration. It can be used in the study of hematologic malignancies and diseases associated with HCN and DRG neurons.No significant effect on protein kinase C (PKC), protein kinase G (PKG) or myosin light chain kinase (MLCK).
Molecular Weight | 537.61 |
Formula | C32H31N3O5 |
CAS Number | 108068-98-0 |
Form | Solid |
Solubility (25°C) | methanol: 5 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Andrew J Murray. Pharmacological PKA inhibition: all may not be what it seems
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