KN-62

• Description:

  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.

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  CaMK II; P2X7 Receptor

• CAS Number:

  127191-97-3