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Purity: ≥98%
KN-62 (KN62; KN 62) is a potent, selective, cell-permeable and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with potential anticancer activity. It inhibits CaMKII with a Ki of 0.9 μM. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca2+-channels. The effect of KN62 on Ca2+-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool.
| ln Vitro |
ATP-stimulated Ba2+ influx into human lymphocytes loaded with fura-2 is potently inhibited by KN-62, with an IC50 of 12.7 nM and total flux suppression at 500 nM[1]. 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[2]. 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[4].
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| ln Vivo |
Five-week-old BALB/c athymic nude mice implanted with TAMR-MCF-7 cells showed a significant reduction in the liver metastatic tumor burden after receiving KN62 (5?mg/kg/day; ip; three times a week for six weeks)[3]. ?ZnCl2 (10 mg/kg, po) does not exhibit antidepressant-like behavior, and KN-62 (1 μg/site, icv) does not either[5].
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| References |
[1]. Gargett CE, et al. The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br J Pharmacol. 1997 Apr;120(8):1483-90.
[2]. H Hidaka, et al. Pharmacology of protein kinase inhibitors. Annu Rev Pharmacol Toxicol. 1992;32:377-97. [3]. Miso Park, et al. Involvement of the P2X7 receptor in the migration and metastasis of tamoxifen-resistant breast cancer: effects on small extracellular vesicles production. Sci Rep. 2019 Aug 12;9(1):11587. [4]. Ravi RG, et al. Potent P2X7 Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach. Drug Dev Res. 2001 Oct;54(2):75-87. [5]. Manosso LM, et al. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Jun 3;59:59-67 |
| Molecular Formula |
C38H35N5O6S2
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| Molecular Weight |
721.84
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| CAS # |
127191-97-3
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| SMILES |
S(C1=C([H])C([H])=C([H])C2C([H])=NC([H])=C([H])C1=2)(N(C([H])([H])[H])[C@@]([H])(C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OS(C1=C([H])C([H])=C([H])C2C([H])=NC([H])=C([H])C1=2)(=O)=O)C(N1C([H])([H])C([H])([H])N(C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H])=O)(=O)=O
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| Chemical Name |
(S)-4-(2-(N-methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl)phenyl isoquinoline-5-sulfonate
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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: ≥ 2.5 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.46 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 25.0 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 | 1.3853 mL | 6.9267 mL | 13.8535 mL | |
| 5 mM | 0.2771 mL | 1.3853 mL | 2.7707 mL | |
| 10 mM | 0.1385 mL | 0.6927 mL | 1.3853 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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