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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Andrew J Murray. Pharmacological PKA inhibition: all may not be what it seems
| Related PKA Products |
|---|
| Malantide
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. |
| PKI (14-24)amide TFA
PKI (14-24)amide TFA is a potent PKA inhibitor. |
| PKA Inhibitor Fragment (6-22) amide
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. |
| PKI (14-24)amide
PKI (14-24)amide is a potent PKA inhibitor. |
| H1-7 (histone H1 phosphorylation site), PKA Substrate
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate. |
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