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

Chemical Properties

Yellow Solid

Uses

Different sources of media describe the Uses of 127191-97-3 differently. You can refer to the following data:
1. A specific inhibitor of Ca2+/Calmodulin-dependent protein kinase II
2. selectively inhibits rat brain Ca2+/cadmodulin-dependent protein kinase II,
3. It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 ?M) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 ?M of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).

General Description

A cell-permeable, reversible, and selective inhibitor of CaM kinase II (Ki = 900 nM for rat brain CaM kinase II) that binds directly to the calmodulin binding site of the enzyme. Also inhibits the growth of K562 cells in a dose-dependent manner.

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