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AB120421

KN-62, CaM kinase II inhibitor. P2X7 antagonist.

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(4 Publications)

MW 721.8 Da, Purity >98%. Cell-permeable, reversible and selective inhibitor of CaM kinase II (IC50 = 500 nM). Interacts with the calmodulin binding site of the enzyme. At higher concentrations reported to inhibit GSK3β, PRAK and MAPKAP-K2. Also potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
2 Images
Immunocytochemistry/ Immunofluorescence - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (AB120421)
  • ICC/IF

Unknown

Immunocytochemistry/ Immunofluorescence - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (AB120421)

ab18197 staining PCNA in SK-N-SH cells treated with KN-62 (ab120421), by ICC/IF. Increase in PCNA nuclear expression correlates with increased concentration of KN-62, as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120421 (KN-62) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab18197 (1 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight® 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

Chemical Structure - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (AB120421)
  • Chemical Structure

Lab

Chemical Structure - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (AB120421)

2D chemical structure image of ab120421, KN-62, CaM kinase II inhibitor. P2X7 antagonist.

Key facts

CAS number

127191-97-3

Purity

>98%

Form

Solid

form

Molecular weight

721.8 Da

Molecular formula

C<sub>3</sub><sub>8</sub>H<sub>3</sub><sub>5</sub>N<sub>5</sub>O<sub>6</sub>S<sub>2</sub>

PubChem

5312126

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

(S)-4-(2-(N-methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl)phenyl isoquinoline-5-sulfonate

Biological description

Cell-permeable, reversible and selective inhibitor of CaM kinase II (IC50 = 500 nM). Interacts with the calmodulin binding site of the enzyme. At higher concentrations reported to inhibit GSK3β, PRAK and MAPKAP-K2. Also potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).

Canonical 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

Isomeric smiles

CN([C@@H](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

InChi

InChI=1S/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

InChiKey

RJVLFQBBRSMWHX-DHUJRADRSA-N

IUPAC Name

[4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate

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Complementary Products

Biochemicals

AB120980

KN-93 (water soluble), CaMK II inhibitor

Immunocytochemistry/ Immunofluorescence - KN-93 (water soluble), CaMK II inhibitor (AB120980)

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Biochemicals

AB120341

H89 dihydrochloride, Kinase inhibitor

Functional Studies - H89 dihydrochloride, Kinase inhibitor (AB120341)

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Biochemicals

AB120413

A 438079, competitive P2X7 receptor antagonist

Chemical Structure - A 438079, competitive P2X7 receptor antagonist (AB120413)

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Primary Antibodies

AB52476

Anti-CaMKII antibody [EP1829Y]

RabMAb|Recombinant

Immunocytochemistry/ Immunofluorescence - Anti-CaMKII antibody [EP1829Y] (AB52476)

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

CaMKII also known as calcium/calmodulin-dependent protein kinase II is a multifunctional serine/threonine kinase. It exists in various isoforms including CaMKII alpha beta and delta which are differentially expressed in tissues like the brain and heart. CaMKII has a molecular mass ranging from approximately 50 to 60 kDa depending on the isoform. P2X7 is a purinergic receptor important in immune system function expressed in tissues such as the brain bone and immune cells. These proteins play vital roles in multiple biological processes by activating and modulating cellular signals.
Biological function summary

CaMKII performs key functions in synaptic plasticity and memory formation in neurons. It forms multi-subunit complexes and undergoes autophosphorylation to sustain its activity. In cardiac muscle CaMKII regulates calcium homeostasis impacting heart muscle contraction. P2X7 receptors are important for mediating ATP-induced cellular processes within immune cells. Their activation leads to the formation of pores that allow ions and molecules to pass through which is vital for inflammasome activation and apoptosis.

Pathways

Both CaMKII and P2X7 plays significant roles in intracellular signal transduction. CaMKII is heavily involved in the CaMK cascade and interacts with other kinases like KN-62 and chemokine pathways. This regulation impacts synaptic responses and cardiac muscle function with CaMKII linking to proteins such as calmodulin and nitric oxide synthase. P2X7 on the other hand affects pathways related to inflammasome assembly interacting with proteins like ASC and caspase-1 which leads to inflammatory responses.

CaMKII associates with conditions such as Alzheimer's disease and cardiac arrhythmias. Aberrant CaMKII activity affects proteins like tau and amyloid-beta contributing to neurodegenerative processes. In the heart excessive activation facilitates arrhythmias interacting with ion channels such as L-type calcium channels. P2X7 receptors connect to disorders like chronic pain and inflammation through its role in mediating immune responses. Altered P2X7 function impacts interleukin cytokines linking to autoimmune diseases and chronic inflammatory conditions.
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Product protocols

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Publications (4)

Recent publications for all applications. Explore the full list and refine your search

Cell reports 34:108899 PubMed33761345

2021

Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.

Applications

Unspecified application

Species

Unspecified reactive species

Kunwei Wu,Wenyan Han,Qingjun Tian,Yan Li,Wei Lu

Cell reports 25:168-182.e6 PubMed30282026

2018

Activity-Dependent Netrin-1 Secretion Drives Synaptic Insertion of GluA1-Containing AMPA Receptors in the Hippocampus.

Applications

Unspecified application

Species

Unspecified reactive species

Stephen D Glasgow,Simon Labrecque,Ian V Beamish,Sarah Aufmkolk,Julien Gibon,Dong Han,Stephanie N Harris,Paul Dufresne,Paul W Wiseman,R Anne McKinney,Philippe Séguéla,Paul De Koninck,Edward S Ruthazer,Timothy E Kennedy

Scientific reports 5:15000 PubMed26449319

2015

Despair-associated memory requires a slow-onset CA1 long-term potentiation with unique underlying mechanisms.

Applications

Unspecified application

Species

Unspecified reactive species

Liang Jing,Ting-Ting Duan,Meng Tian,Qiang Yuan,Ji-Wei Tan,Yong-Yong Zhu,Ze-Yang Ding,Jun Cao,Yue-Xiong Yang,Xia Zhang,Rong-Rong Mao,Gal Richter-Levin,Qi-Xin Zhou,Lin Xu

Proceedings of the National Academy of Sciences of 111:4321-6 PubMed24599589

2014

Developmental switch in the kinase dependency of long-term potentiation depends on expression of GluA4 subunit-containing AMPA receptors.

Applications

Unspecified application

Species

Unspecified reactive species

Natalia V Luchkina,Johanna Huupponen,Vernon R J Clarke,Sarah K Coleman,Kari Keinänen,Tomi Taira,Sari E Lauri
View all publications
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