Fig. 1 · Structure

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KN-62

Cat. No. A11473 CAS 127191-97-3

CaM kinase II inhibitor

KN-62 is a selective, cell-permeable inhibitor of CaM kinase II.

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Biological Activity

Target & Activity

Target Activity Value
CaMKII Ki 0.9 μM

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 IC50 0.158 μM Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay [PMID: 25597334]
HEK293 IC50 0.25 μM Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium ion uptake after 2 hrs [PMID: 26547056]
HEK293 IC50 158 nM Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced accumulation of ethidium+ after 120 mins by fluorescence assay [PMID: 24246730]
HEK293 IC50 280 nM Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence analysis [PMID: 22400713]
HEK293 IC50 96 μM Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence assay [PMID: 28126517]
THP-1 IC50 0.129 μM Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA [PMID: 26547056]
THP-1 IC50 0.143 μM Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA [PMID: 25597334]
THP-1 IC50 120 nM Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA [PMID: 22400713]
THP-1 IC50 188 nM Inhibition of BzATP-stimulated IL1-beta release in human THP1 cells by ELISA [PMID: 18078749]
THP-1 IC50 81 nM Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA [PMID: 19110420]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 127191-97-3
Applications CaM kinase II inhibitor
Formula C38H35N5O6S2
Molecular Weight 721.8
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

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 96 mg/mL (132.99 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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