KN-62

SKU: orb1226628

Description

KN-62 is a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK II) with Ki of 900 nM for rat brain CaMK II; potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with IC50 of 12.7 nM, inhibits ATP-stimulated ethidium+ uptake with IC50 of 13.1 nM; causes hypertension and tachycardia in rats, associated with the diminished rate of GABA release in cerebrospinal fluid.

Key Properties

• CAS Number: 127191-97-3
• MW: 721.9
• Purity: >98% (HPLC)
• Formula: C₃₈H₃₅N₅O₆S₂
• 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
• Target: CaMK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  KN62 (5 mg/kg/day; ip; three times a week for 6 weeks) significantly reduces the liver metastatic tumor burden in five weeks old BALB/c athymic nude mice inoculated with TAMR-MCF-7 cells. KN-62 (1 μg/site, i. c. v.) prevents the antidepressant-like behavior and antidepressant-like behaviors of ZnCl2 (10 mg/kg, p.o.).
• In Vitro:
  KN-62 potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with an IC50 of 12.7 nM and complete inhibition of the flux at a concentration of 500 nM. KN-62 does not inhibit the activity of autophosphorylated Ca2+/CaM kinase II. KN-62 inhibits the Ca2+/calmodulin-dependent autophosphorylation of both alpha (50 kDa) and beta (60 kDa) subunits of Ca2+/CaM kinase II dose dependently in the presence or absence of exogenous substrate. In human leukemic B lymphocytes, KN-62 reduces the rate of permeability increase to larger permeant cations, like ethidium, induced by Bz-ATP with an IC50 of 13.1 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KN 62 | KN62

Quick Database Links

Gene Symbol

CaMK