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| 5mg |
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| 25mg |
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Purity: ≥98%
KN-93 is a potent, cell-permeable, reversible and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, and with no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 suppresses ventricular arrhythmia induced by LQT2 without decreasing TDR. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. KN-93 ameliorates levodopa-induced dyskinesia in a rat model of Parkinson's disease. KN-93 protects rat cerebral cortical neurons from N-methyl-D-aspartic acid-induced injury.
| ln Vitro |
Following two days of KN-93 treatment, 95% of cells exhibit G1 arrest. G1 arrest is reversible; a peak of cells had proceeded into S and G2-M one day after KN-93 release. In NIH 3T3 fibroblasts, KN-93 also inhibits the development of cells that are stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor[1]. The H+, K+-ATPase activity is inhibited by KN-93, but the proton gradient created in the gastric membrane vesicles is strongly dissipated, and the luminal space volume is decreased[2]. Increased left ventricular developed pressure during action potential extension and early afterdepolarizations is prevented by KN-93 (0.5 μM). Early afterdepolarizations cause a rise in Ca2+-independent CaM kinase activity, which KN -93 blocks[3]. KN-93 (10 μM) dramatically suppresses the increased glucose-induced CaMKII/NF-κB signaling, which in turn reduces Müller cell production of VEGF, iNOS, and ICAM-1[4].
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| ln Vivo |
KN-93 (1 mg/kg/day, ip) decreases phosphorylation of CaMKII and NF-κB in diabetic retina and inhibits retinal vascular leakage caused by diabetes[4].
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| Animal Protocol |
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| References |
[1]. Tombes RM, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK (the multifunctional Ca2+/CaM kinase). Cell Growth Differ. 1995 Sep;6(9):1063-70.
[2]. Mamiya N, et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitorKN-93. Biochem Biophys Res Commun. 1993 Sep 15;195(2):608-15. [3]. Anderson ME, et al. KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006. [4]. Li J, et al. Curcumin Attenuates Retinal Vascular Leakage by Inhibiting Calcium/Calmodulin-Dependent Protein Kinase II Activity in Streptozotocin-Induced Diabetes. Cell Physiol Biochem. 2016;39(3):1196-208 |
| Molecular Formula |
C26H29CLN2O4S
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| Molecular Weight |
501.04
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| CAS # |
139298-40-1
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| Related CAS # |
KN-93 hydrochloride;1956426-56-4;KN-93 phosphate;1913269-12-1
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])/C(/[H])=C(\[H])/C([H])([H])N(C([H])([H])[H])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1N(C([H])([H])C([H])([H])O[H])S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])(=O)=O
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| InChi Key |
LLLQTDSSHZREGW-AATRIKPKSA-N
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| InChi Code |
InChI=1S/C26H29ClN2O4S/c1-28(17-5-6-21-9-11-23(27)12-10-21)20-22-7-3-4-8-26(22)29(18-19-30)34(31,32)25-15-13-24(33-2)14-16-25/h3-16,30H,17-20H2,1-2H3/b6-5+
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| Chemical Name |
(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9958 mL | 9.9792 mL | 19.9585 mL | |
| 5 mM | 0.3992 mL | 1.9958 mL | 3.9917 mL | |
| 10 mM | 0.1996 mL | 0.9979 mL | 1.9958 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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