KN-93

SKU: orb1305151

Description

KN-93 is a cell-permeable, selective inhibitor of Ca²⁺/calmodulin-dependent kinase II (CaMKII) that acts by competitively antagonizing calmodulin binding. It is widely used in vitro and in vivo to investigate CaMKII's roles in cardiac function, neuronal signaling, and synaptic plasticity.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 139298-40-1
• MW: 501.04
• Purity: 99.95% (May vary between batches)
• Formula: C₂₆H₂₉ClN₂O₄S
• SMILES: N(S(=O)(=O)C1=CC=C(OC)C=C1)(CCO)C2=C(CN(CC=CC3=CC=C(Cl)C=C3)C)C=CC=C2
• Target: Autophagy,CaMK
• Solubility: 10% DMSO+90% Corn Oil:1 mg/mL (2 mM);DMSO:50 mg/mL (99.79 mM)

Bioactivity

• Target IC50:
  CaMK II:370 nM. (Ki)
• In Vivo:
  KN-93, administered intraperitoneally at a dosage of 1 mg/kg/day, effectively reduces retinal vascular leakage in diabetes and concurrently inhibits the phosphorylation of CaMKII and NF-κB within the diabetic retina.
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• In Vitro:
  Following 2 days of treatment with KN-93, 95% of cells are halted in the G1 phase, a process which is reversible; one day post KN-93 withdrawal, a notable number of cells transition into the S and G2-M phases. KN-93 effectively inhibits cell growth prompted by various growth factors, including basic fibroblast growth factor, platelet-derived growth factor-BB, epidermal growth factor, and insulin-like growth factor-1, in NIH 3T3 fibroblasts. Moreover, KN-93 disrupts H+, K+-ATPase activity, significantly dissipates the proton gradient across gastric membrane vesicles, and diminishes the luminal space volume. At a concentration of 0.5 μM, KN-93 averts the increase in left ventricular (LV) developed pressure and the occurrence of early afterdepolarizations. It also blocks the rise in Ca2+-independent CaM kinase activity observed during these afterdepolarizations. At a 10 μM concentration, KN-93 significantly suppresses the activation of CaMKII/NF-κB signaling triggered by high glucose levels, leading to a decreased expression of VEGF, iNOS, and ICAM-1 in Müller cells.
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• Cell Research:
  KN-93 is dissolved in DMSO. Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150 μL DMSO. The optical density of the solution is measured at 490 nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group).
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Storage & Handling

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

Alternative Names

Autophagy, CaMK, Calmodulin-dependent protein kinases, Calmodulin-dependent kinases, Inhibitor, inhibit, KN93, KN-93, KN 93

Compound Identifiers

PubChem CID

3837