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  1. Link

    products/biochemicals/kn-62-cam-kinase-ii-inhibitor-p2x7-antagonist-ab120421.pdf

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KN-62, CaM kinase II inhibitor. P2X7 antagonist. (ab120421)

  • Datasheet
  • COA
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Chemical Structure - KN-62, CaM kinase II inhibitor. P2X<sub>7</sub> antagonist. (ab120421)
  • Immunocytochemistry/ Immunofluorescence - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (ab120421)

Key features and details

  • CaM kinase II inhibitor. P2X7 antagonist.
  • CAS Number: 127191-97-3
  • Purity: > 98%
  • Soluble in DMSO to 100 mM
  • Form / State: Solid
  • Source: Synthetic

Overview

  • Product name

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

    CaM kinase II inhibitor. P2X7 antagonist.
  • 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).

  • Purity

    > 98%
  • CAS Number

    127191-97-3
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    4-[(2S)-2-[(5-Isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenylisoquinolinesulfonic acid ester
  • Molecular weight

    721.84
  • Molecular formula

    C38H35N5O6S2
  • PubChem identifier

    5312126
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    O=C([C@H](Cc3ccc(OS(=O)(=O)c2cccc1cnccc12)cc3)N(C)S(=O)(=O)c5cccc4cnccc45)N6CCN(CC6)c7ccccc7
  • Source

    Synthetic

  • Research areas

    • Cell Biology
    • Cell Cycle
    • Kinases/Phosphatases
    • Other
    • Neuroscience
    • Neurotransmission
    • Intracellular Signaling
    • Kinases
    • Neuroscience
    • Neurotransmission
    • Calcium Signaling
    • Calmodulin / CaMK
    • Neuroscience
    • Cell Type Marker
    • Neuron marker
    • Soma marker
    • Neuroscience
    • Neurotransmission
    • Receptors / Channels
    • Ligand-Gated Ion Channels
    • P2X Receptors
    • Signal Transduction
    • Protein Phosphorylation
    • Ser / Thr Kinases
    • Other Kinases
    • Signal Transduction
    • Signaling Pathway
    • Calcium Signaling
    • Calmodulin Pathway
    • Epigenetics and Nuclear Signaling
    • Cell cycle
    • Kinases/Phosphatases
    • Other
    • Cardiovascular
    • Heart
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    • Hypertrophy
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    • Receptors & Transporters
    • Purinergics
    • P2
    • P2X
    • Antagonists
    • Metabolism
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    • Metabolic signaling pathways
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    • Metabolism processes
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    • CAM Kinase
    • Biochemicals
    • Research Area
    • Cancer
    • Ca2+ signaling
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Applications

The Abpromise guarantee

Our Abpromise guarantee covers the use of ab120421 in the following tested applications.

The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.

Application Abreviews Notes
Functional Studies
Use at an assay dependent concentration.
Notes
Functional Studies
Use at an assay dependent concentration.

Images

  • Chemical Structure - KN-62, CaM kinase II inhibitor. P2X<sub>7</sub> antagonist. (ab120421)
    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.
  • Immunocytochemistry/ Immunofluorescence - KN-62, CaM kinase II inhibitor. P2X7 antagonist. (ab120421)
    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.

Protocols

To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.

Click here to view the general protocols

Datasheets and documents

  • Datasheet download

    Download
  • COA

References (4)

Publishing research using ab120421? Please let us know so that we can cite the reference in this datasheet.

ab120421 has been referenced in 4 publications.

  • Wu K  et al. Activity- and sleep-dependent regulation of tonic inhibition by Shisa7. Cell Rep 34:108899 (2021). PubMed: 33761345
  • Glasgow SD  et al. Activity-Dependent Netrin-1 Secretion Drives Synaptic Insertion of GluA1-Containing AMPA Receptors in the Hippocampus. Cell Rep 25:168-182.e6 (2018). PubMed: 30282026
  • Jing L  et al. Despair-associated memory requires a slow-onset CA1 long-term potentiation with unique underlying mechanisms. Sci Rep 5:15000 (2015). PubMed: 26449319
  • Luchkina NV  et al. Developmental switch in the kinase dependency of long-term potentiation depends on expression of GluA4 subunit-containing AMPA receptors. Proc Natl Acad Sci U S A 111:4321-6 (2014). PubMed: 24599589

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