Name | KN-93 |
Synonyms | KN-93 KN-93, WATER-SOLUBLE METHOXYBENZENE-SULFONAMIDE 2-[N-(2-HYDROXYETHYL)-N-(4-METHOXYBENZENESULFONYL)]AMINO-N-(4-CHLOROCINNAMYL)-N-METHYLBENZYLAMINE N-[2-N-4-CHLOROCINNAMYL-N-METHYLAMINOMETHYLPHENYL]-N-[2-HYDROXYETHYL]-4-METHOXYBENZENESULFONAMIDE N-[2-[[[3-(4-CHLOROPHENYL)-2-PROPENYL]METHYLAMINO]METHYL]PHENYL]-N-(2-HYDROXYETHYL)-4-METHOXYBENZENESULPHONAMIDE N-[2-[[[3-(4'-CHLOROPHENYL)-2-PROPENYL]METHYLAMINO]METHYL]PHENYL]-N-(2-HYDROXYETHYL)-4'-METHOXY-BENZENESULFONAMIDE PHOSPHATE |
CAS | 139298-40-1 |
InChIKey | LLLQTDSSHZREGW-AATRIKPKSA-N |
Molecular Formula | C26H29ClN2O4S |
Molar Mass | 501.04 |
Density | 1.288 |
Solubility | DMSO: 1mg/mL |
Appearance | Off-white solid |
Color | white |
Storage Condition | 2-8°C |
In vitro study | After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts. KN-93 inhibits the H + , K + -ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca 2+ -independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells. |
In vivo study | KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37 - Wear suitable protective clothing and gloves. |
WGK Germany | 3 |
HS Code | 29299000 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.996 ml | 9.979 ml | 19.958 ml |
5 mM | 0.399 ml | 1.996 ml | 3.992 ml |
10 mM | 0.2 ml | 0.998 ml | 1.996 ml |
5 mM | 0.04 ml | 0.2 ml | 0.399 ml |
biological activity | KN-93 is a cell-permeable and competitive Ca2 /calmodulin-dependent protein kinase II (CaMK-II) the Ki value of the reversible inhibitor of CaM Kinase activity for rabbit myocardium was 2.58 μm. |
Target | Value |
CaMKII (Cell-free assay) | 2.58 μM(Ki) |