KN-62

KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.

Product Specifications

CAS Number

[127191-97-3]

UNSPSC

12352005

Target

CaMK; P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-Kinase/protease

Field of Research

Metabolic Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/KN-62.html

Purity

99.23

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(N1CCN(C2=CC=CC=C2)CC1)[C@H](CC3=CC=C(C=C3)OS(=O)(C4=CC=CC5=C4C=CN=C5)=O)N(C)S(=O)(C6=CC=CC7=C6C=CN=C7)=O

Molecular Formula

C38H35N5O6S2

Molecular Weight

721.84

References & Citations

[1]Gargett CE, et al. The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br J Pharmacol. 1997 Apr;120 (8) :1483-90.|[2]Ravi RG, et al. Potent P2X7 Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach. Drug Dev Res. 2001 Oct;54 (2) :75-87.|[3]Manosso LM, et al. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Jun 3;59:59-67.|[4]H Hidaka, et al. Pharmacology of protein kinase inhibitors. Annu Rev Pharmacol Toxicol. 1992;32:377-97.|[5]Miso Park, et al. Involvement of the P2X7 receptor in the migration and metastasis of tamoxifen-resistant breast cancer: effects on small extracellular vesicles production. Sci Rep. 2019 Aug 12;9 (1) :11587.