KT5720 

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].

IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 µM (PKA)^[3].

KT5720 (0-8 μM; 72 h) reverses multidrug resistance in an MDR1 lymphoma cell model^[1].
? KT5720 (3 μM) attenuates I_h 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KT5720 (5 mg/kg; i.p.; single daily for 8 days) reverses completely DNR resistance in MDR1 transgenic mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

537.61

C₃₂H₃₁N₃O₅

108068-98-0

Solid

White to off-white

C[C@@]12N3C4=C(C5=CC=CC=C35)C(CNC6=O)=C6C7=C4N(C8=CC=CC=C87)[C@@](C[C@@]2(O)C(OCCCCCC)=O)([H])O1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]