KN-62, CaM kinase II inhibitor. P2X7 antagonist.
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(4 제품이 사용된 논문 )
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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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
- 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
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.
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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.
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This supplementary information is collated from multiple sources and compiled automatically.
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.
제품이 사용된 논문 (4)
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Cell reports 34:108899 PubMed33761345
2021
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Cell reports 25:168-182.e6 PubMed30282026
2018
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Scientific reports 5:15000 PubMed26449319
2015
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Proceedings of the National Academy of Sciences of 111:4321-6 PubMed24599589
2014
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