127191-97-3

Basic information

• Product Name: KN-62
• Synonyms: 1-(N,O-BIS-(5-ISOQUINOLINESULFONYL)-*N-M ETHYL-L-TYR;KN-62 97%;KN-62, 99+%;4-((2S)-2-((5-isoquinolinylsulfonyl)methylamino)-3-oxo-3-(4-phenyl-1-piperazinyl)propyl)phenylisoquinolinesulfonicacid;1-(N,O-Bis-[5-isoquinolinesulfonyl]-N-methyl-L-tyrosyl)-4-phenylpiperazine, (S)-5-Isoquinolinesulfonic Acid 4-(2-[(5-Isoquinolinylsulfonyl)methylamino]- 3-oxo-3-[4-phenyl-1-piperazinyl]propyl)phenyl Ester,;5-Isoquinolinesulfonic acid, 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester;(s)-5-isoquinolinesulfonic acid 4-[2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl ester;(1-(N,O-BIS-(5-ISOQUINOLINESULFONYL)-N-METHYL-L-TYROSYL)4-PHENYLPIPERAZINE) KN 62
• CAS NO: 127191-97-3
• Molecular Formula: C38H35N5O6S2
• Molecular Weight: 721.84
• Product Categories: Protein Kinase Inhibitors and Activators;Protein Kinase;Inhibitor
• Mol File: 127191-97-3.mol
• Article Data: 0

Chemical Properties

• Melting Point: 92-94°C
• Boiling Point: 964.731 °C at 760 mmHg
• Flash Point: 537.25 °C
• Appearance: white/solid
• Density: 1.388
• Vapor Pressure: 0mmHg at 25°C
• Refractive Index: 1.685
• Storage Temp.: −20°C
• Solubility: 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.93 mg/m
• PKA: 4.07±0.13(Predicted)
• CAS DataBase Reference: KN-62(CAS DataBase Reference)
• NIST Chemistry Reference: KN-62(127191-97-3)
• EPA Substance Registry System: KN-62(127191-97-3)

Safety Data

• Safety Statements: 24/25
• WGK Germany: 3
• Hazardous Substances Data: 127191-97-3(Hazardous Substances Data)

Usage

Description

KN-62 is a cell-permeable, reversible, and selective inhibitor of CaM kinase II (CaMKII) with a Ki value of 900 nM for rat brain CaM kinase II. It is a yellow solid that binds directly to the calmodulin binding site of the enzyme, thereby inhibiting its activity.

Uses

Used in Neuroscience Research:
KN-62 is used as a potent and selective inhibitor of CaMKII for studying the role of this enzyme in various cellular processes. It has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II, causing cells to arrest in the S phase.
Used in Cell Cycle Regulation Studies:
KN-62 is used as a tool to investigate the role of CaMKII in cell cycle regulation. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 μM of KN-62 blocked CaMKII phosphorylation of III-AC and inhibited hormone-stimulated Ca2+ oscillations.
Used in P2X7 Receptor Research:
KN-62 is used as a potent non-competitive antagonist at the P2X7 receptor with an IC50 value of 15 nM. This application allows researchers to study the effects of P2X7 receptor modulation on various physiological processes.
Used in Cancer Research:
KN-62 is used to study its effects on the growth of K562 cells in a dose-dependent manner, providing insights into the potential role of CaMKII inhibition in cancer therapy.
Used in Pharmaceutical Development:
KN-62 serves as a starting point for the development of new drugs targeting CaMKII, which may have therapeutic applications in various diseases, including cancer and neurological disorders.

Biological Activity

Selective, cell-permeable inhibitor of CaM kinase II (IC 50 = 0.9 μ M). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X 7 receptor (IC 50 = 15 nM). Also available as part of the Mixed Kinase Inhibitor Tocriset? .

Biochem/physiol Actions

Selectively inhibits rat brain Ca2+/calmodulin-dependent protein kinase II.

InChI:InChI=1/C38H35N5O6S2/c1-41(50(45,46)36-11-5-7-29-26-39-19-17-33(29)36)35(38(44)43-23-21-42(22-24-43)31-9-3-2-4-10-31)25-28-13-15-32(16-14-28)49-51(47,48)37-12-6-8-30-27-40-20-18-34(30)37/h2-20,26-27,35H,21-25H2,1H3/t35-/m0/s1