| Bioactivity | KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 µM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases[1][2][3]. | |||||||||
| Target | IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 µM (PKA). | |||||||||
| Invitro | KT5720 (0-8 µM; 72 h) reverses multidrug resistance in an MDR1 lymphoma cell model[1].KT5720 (3 µM) attenuates Ih in freshly isolated rat DRG neurons and slows down HCN channel activation kinetics[2].KT5720 (3 µM) reduces DRG neurons excitability and reduces DRG neuron intracellular Ca2 + level[2]. Cell Viability Assay[1] Cell Line: | |||||||||
| In Vivo | KT5720 (5 mg/kg; i.p.; single daily for 8 days) reverses completely DNR resistance in MDR1 transgenic mice model[1]. Animal Model: | |||||||||
| Name | KT5720 | |||||||||
| CAS | 108068-98-0 | |||||||||
| Formula | C32H31N3O5 | |||||||||
| Molar Mass | 537.61 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Galski H, et al. In vitro and in vivo reversal of MDR1-mediated multidrug resistance by KT-5720: implications on hematological malignancies. Leuk Res. 2006 Sep;30(9):1151-8. [2]. Cheng Q, et al. Novel role of KT5720 on regulating hyperpolarization-activated cyclic nucleotide-gated channel activity and dorsal root ganglion neuron excitability. DNA Cell Biol. 2013 Jun;32(6):320-8. [3]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. |