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
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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).
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Purity
> 98% -
CAS Number
127191-97-3 -
Chemical structure
Properties
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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.
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SMILES
O=C([C@H](Cc3ccc(OS(=O)(=O)c2cccc1cnccc12)cc3)N(C)S(=O)(=O)c5cccc4cnccc45)N6CCN(CC6)c7ccccc7 -
Source
Synthetic
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Research areas
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.
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| Notes |
|---|
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Functional Studies
Use at an assay dependent concentration. |
Images
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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.
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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.
References (4)
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
