GLPBio

KN-62

Catalog No.: GC14202Purity:>99.00%
COASDSData Sheet
KN-62 is a selective calmodulin-dependent protein kinase II (CaMKII) inhibitor and also a potent non-competitive P2X7 receptor antagonist.

Products are for research use only. Not for human use. We do not sell to patients.

KN-62
Cas No.: 127191-97-3
10mM (in 1mL DMSO)In Stock
$89.00
1
1mgIn Stock
$26.00
1
5mgIn Stock
$56.00
1
10mgIn Stock
$95.00
1
50mgIn Stock
$385.00
1
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Description

KN-62 is a selective calmodulin-dependent protein kinase II (CaMKII) inhibitor and also a potent non-competitive P2X7 receptor antagonist[1][2]. CaMKII is a serine/threonine kinase that plays a critical role in calcium signaling by phosphorylating various substrates involved in neurotransmission, muscle contraction, and other cellular processes[3]. P2X7 is an ATP-gated ion channel belonging to the P2X receptor family, which is activated by high concentrations of extracellular ATP and mediates inflammatory responses and cell death[4]. KN-62 is usually used in the research of neural signal transduction, inflammatory response and tumor metastasis mechanisms[5].

In vitro, treatment of tamoxifen-resistant MCF-7 cells with KN-62 (3μM; 24h) inhibits ATP-induced calcium influx, cell proliferation and migration, and reduces small extracellular vesicle secretion and CD63 expression[6].

In vivo, KN-62 (1μg/site; i.c.v.) reversed the ZnCl₂-induced reduction in immobility time in the tail suspension test in Swiss mice[7].

References:
[1] Schweitzer ES, Sanderson MJ, Wasterlain CG. Inhibition of regulated catecholamine secretion from PC12 cells by the Ca2+/calmodulin kinase II inhibitor KN-62. J Cell Sci. 1995;108 ( Pt 7):2619-2628.
[2] Gargett CE, Wiley JS. The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br J Pharmacol. 1997;120(8):1483-1490.
[3] Reyes Gaido OE, Nkashama LJ, Schole KL, et al. CaMKII as a Therapeutic Target in Cardiovascular Disease. Annu Rev Pharmacol Toxicol. 2023;63:249-272.
[4] Sluyter R. The P2X7 Receptor. Adv Exp Med Biol. 2017;1051:17-53.
[5] Pellicena P, Schulman H. CaMKII inhibitors: from research tools to therapeutic agents. Front Pharmacol. 2014;5:21.
[6] Park M, Kim J, Phuong NTT, et al. Involvement of the P2X7 receptor in the migration and metastasis of tamoxifen-resistant breast cancer: effects on small extracellular vesicles production. Sci Rep. 2019;9(1):11587.
[7] Manosso LM, Moretti M, Ribeiro CM, Gonçalves FM, Leal RB, Rodrigues ALS. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015;59:59-67.

Protocol

Cell experiment [1]:

Cell lines

TAMR-MCF-7 cells

Preparation Method

TAMR-MCF-7 cells were cultured at 37°C in 5% CO2/95% air in Dulbecco’s modified Eagle’s medium (DMEM) containing 10% fetal bovine serum (FBS) and antibiotics. 5×104 cells were seeded in 96 well-plate, and cells were treated with 3μM KN-62 and 100μM ATP for 24h. The phase percentage of cells were scanned every 4h by using the IncuCyte ZOOMTM Live Cell Anaylsis System. The intracellular calcium contents were measured using a FlexStation scanning fluorimeter with an integrated fluid transfer workstation. Cell migration assay was quantified by both trans-well migration and wound healing assays. And cells were collected for further Western blot and RT-PCR analyses.

Reaction Conditions

3μM; 24h

Applications

Treatment of tamoxifen-resistant MCF-7 cells with KN-62 inhibits ATP-induced calcium influx, cell proliferation and migration, and reduces CD63 expression.
Animal experiment [2]:

Animal models

Female Swiss mice

Preparation Method

Female Swiss mice (45–55 days old, weighing 30–45g) were maintained at 20–22°C with free access to water and food, under a 12:12h light:dark cycle (lights on at 7:00 a.m.). The animals were caged in groups of 15 in a 41×34×16-cm cage. All behavioral tests were carried out between 9:00 a.m. and 04:00 p.m. Animals were acclimatized to the laboratory for at least 12h before testing. Mice were pretreated with an effective dose of ZnCl2 (10mg/kg, p.o.), and 30min later they received (i.c.v.) 1μg/site KN-62. The animals were submitted to behavioral tests 30min later (60min after zinc administration). The number of animals used for behavioral tests was 7–8 per group. The total duration of immobility induced by tail suspension was measured. Mice both acoustically and visually isolated were suspended 50cm above the floor by adhesive tape placed approximately 1cm from the tip of the tail. Mice were considered immobile only when they hung passively and completely motionless. The immobility time was recorded during a 6-min period by an experienced observer. A decreased immobility time was considered indicative of an antidepressant-like effect.

Dosage form

1μg/site; i.c.v.

Applications

KN-62 reversed the ZnCl₂-induced reduction in immobility time in the tail suspension test in Swiss mice.

References:
[1] Park M, Kim J, Phuong NTT, et al. Involvement of the P2X7 receptor in the migration and metastasis of tamoxifen-resistant breast cancer: effects on small extracellular vesicles production. Sci Rep. 2019;9(1):11587.
[2] Manosso LM, Moretti M, Ribeiro CM, Gonçalves FM, Leal RB, Rodrigues ALS. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015;59:59-67.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
127191-97-3
Chemical Name
[4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate
SMILES
CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7
Molecular Formula
C38H35N5O6S2
Molecular Weight
721.9
Solubility
≥ 36.1mg/mL in DMSO, ≥ 15.88 mg/mL in EtOH with ultrasonic
Storage
Desiccate at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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