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Purity: ≥98%
KN-93 Phosphate (KN 93; KN93), the phosphate salt of KN-93, is a potent, cell-permeable and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with potential anti-Parkinson's disease and anticancer activity. It inhibits CaMKII with a Ki of 0.37 μM, and showed no 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 |
Ninety-five percent of the cells were in the G1 phase after two days of treatment with KN-93 phosphate. G1 arrest is reversible, and cells peak into the S and G2-M phases one day after KN-93 phosphate is released. KN-93 phosphate also inhibits the proliferation of NIH 3T3 fibroblasts when they are stimulated by platelet-derived growth factor-BB, epidermal growth factor, and basic fibroblast growth factor [1]. While KN-93 phosphate strongly dissipates the proton gradient produced in stomach membrane vesicles and decreases cavity volume, it also inhibits the action of H+ and K+-ATPase [2]. Preventing LV developmental stress rises during action potential extension and early afterdepolarization is possible with KN-93 phosphate (0.5 μM). Early afterdepolarization is characterized by a rise in Ca2+-independent CaM kinase activity, which is inhibited by KN-93 phosphate [3].
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| References |
Biochem Biophys Res Commun.1991 Dec 31;181(3):968-75;Neuropsychiatr Dis Treat.2013;9:1213-20.
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| Molecular Formula |
C26H32CLN2O8PS
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| Molecular Weight |
599.03
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| Exact Mass |
598.131
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| CAS # |
1188890-41-6
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| Related CAS # |
KN-93;139298-40-1;KN-93 hydrochloride;1956426-56-4
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| PubChem CID |
16760530
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| Appearance |
White to off-white solid powder
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| LogP |
4.833
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
763
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C/C=C/C1=CC=C(C=C1)Cl)CC2=CC=CC=C2N(CCO)S(=O)(=O)C3=CC=C(C=C3)OC.OP(=O)(O)O
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| InChi Key |
NNKJTPOXLIILMB-IPZCTEOASA-N
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| InChi Code |
InChI=1S/C26H29ClN2O4S.H3O4P/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;1-5(2,3)4/h3-16,30H,17-20H2,1-2H3;(H3,1,2,3,4)/b6-5+;
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| Chemical Name |
(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6694 mL | 8.3468 mL | 16.6937 mL | |
| 5 mM | 0.3339 mL | 1.6694 mL | 3.3387 mL | |
| 10 mM | 0.1669 mL | 0.8347 mL | 1.6694 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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