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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
| Related PKA Products |
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| H-89 Dihydrochloride
H-89 dihydrochloride is a selective inhibitor of protein kinase A (PKA) with an IC50 value of 135 nM. |
| Bucladesine Sodium Salt
Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. |
| H-89
H-89 is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
| 8-Bromo-cAMP sodium salt
8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator. |
| 5-Iodotubercidin
5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. |
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