108068-98-0
Chemical Structure
KT5720
- CAS No.: 108068-98-0
- Formula:C32H31N3O5
- Molecular Weight:537.61
IUPAC Name: hexyl (5R,6S,8S)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate
InChIKey: ZHEHVZXPFVXKEY-RUAOOFDTSA-N
SMILES: 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
Biological Activity: 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].
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KT5720 | 98.53% | 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. | ||||||||||||||||||||
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References
- [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]
