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).
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- Cell reports 34:1088992021Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKunwei Wu,Wenyan Han,Qingjun Tian,Yan Li,Wei LuPubMed 33761345
- Cell reports 25:168-182.e62018Activity-Dependent Netrin-1 Secretion Drives Synaptic Insertion of GluA1-Containing AMPA Receptors in the Hippocampus.Applications:Unspecified applicationReactive species:Unspecified reactive speciesStephen 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 KennedyPubMed 30282026
- Scientific reports 5:150002015Despair-associated memory requires a slow-onset CA1 long-term potentiation with unique underlying mechanisms.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLiang Jing et. al.PubMed 26449319
- Proceedings of the National Academy of Sciences of 111:4321-62014Developmental switch in the kinase dependency of long-term potentiation depends on expression of GluA4 subunit-containing AMPA receptors.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNatalia V Luchkina et. al.PubMed 24599589
Key facts
- CAS number
- 127191-97-3
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 721.8 Da
- Molecular formula
- C38H35N5O6S2
- PubChem identifier
- 5312126
- Nature
- Synthetic
Target data
Alternative names
ATP receptor, Alpha CaMKII, CAM 2, CAM kinase 2 delta, CAM kinase II delta, CAMK 2, CAMK 2B, CAMK 2d, CAMK II, CAMK2G, CAMKA, CAMKB, CAMKD, CAMKI, CaM kinase II, CaM kinase II alpha, CaM kinase II alpha chain, CaM kinase II alpha subunit, CaM kinase II beta, CaM kinase II beta subunit, CaM kinase II delta subunit, CaM kinase II gamma, CaM kinase II subunit alpha, CaM kinase II subunit beta, CaM kinase II subunit delta, CaM-kinase II beta chain, CaM-kinase II delta chain, CaMK II alpha subunit, CaMK II beta subunit, CaMK-II delta subunit, CaMK-II subunit alpha, CaMK-II subunit beta, CaMK-II subunit delta, CaMK2 beta, CaMKIIB, CaMKIINalpha, Calcium / calmodulin dependent protein kinase 2 delta, Calcium / calmodulin dependent protein kinase II delta, Calcium calmodulin dependent protein kinase II, Calcium/calmodulin dependent protein kinase (CaM kinase) II beta, Calcium/calmodulin dependent protein kinase II alpha B subunit, Calcium/calmodulin dependent protein kinase II gamma, Calcium/calmodulin dependent protein kinase IIB, Calcium/calmodulin dependent protein kinase type II alpha chain, Calcium/calmodulin dependent protein kinase type II beta chain, Calcium/calmodulin-dependent protein kinase (CaM kinase) II alpha, Calcium/calmodulin-dependent protein kinase II-alpha, Calcium/calmodulin-dependent protein kinase type II subunit alpha, Calcium/calmodulin-dependent protein kinase type II subunit beta, Calcium/calmodulin-dependent protein kinase type II subunit delta, Calcium/calmodulin-dependent protein kinase type IIA, Camk2a, EC 2.7.11.17, KCC2A_HUMAN, KCC2B_HUMAN, KCC2D_HUMAN, KIAA0968, MGC123320, MGC139375, MGC155201, MGC29528, P2RX7_HUMAN, P2X purinoceptor 7, P2Z receptor, PK2CDD, PKCCD, Purinergic receptor, R74975, RATCAMKI, calcium/calmodulin-dependent protein kinase (CaM kinase) II delta, calcium/calmodulin-dependent protein kinase II beta, calcium/calmodulin-dependent protein kinase type II delta chain, mKIAA0968, proline rich calmodulin-dependent protein kinase, purinergic receptor P2X, ligand gated ion channel, 7, zgc:112538, zgc:123320
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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).
Key facts
- CAS number
- 127191-97-3
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 721.8 Da
- Molecular formula
- C38H35N5O6S2
- PubChem identifier
- 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
Storage
- 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
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
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.
- Associated diseases and disorders
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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2 product images
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)
Anti-PCNA antibody 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 Anti-PCNA antibody 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 (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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