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].

Product Specifications

CAS Number

[108068-98-0]

UNSPSC

12352005

Hazard Statement

H370

Target

PKA

Type

Reference compound

Related Pathways

Stem Cell/Wnt; TGF-beta/Smad

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/kt5720.html

Purity

99.0

Solubility

Methanol : 5 mg/mL (ultrasonic;warming)

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

Molecular Formula

C32H31N3O5

Molecular Weight

537.61

Precautions

H370

References & Citations

[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.