KN-92 hydrochloride |
| Catalog No.GC15988 |
An inactive control compound for a CaMKII inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1431698-47-3
Sample solution is provided at 25 µL, 10mM.
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KN-92 is an inactive analog of KN-93. KN-93 is the CaM kinase II inhibitor. [1]
Hearts were treated with the CaM kinase inhibitor KN-93 or the inactive analog KN-92 (0.5 μM) for 10 min before clofilium exposure. Early afterdepolarizations (EADs) were largely inhibited by KN-93 contrasted to KN-92. There were little differences in parameters favoring EADs such as monophasic action potential duration or heart rate in KN-92- or KN-93- treated hearts. CaM kinase activity in situ increased 37% in hearts with EADs compared to hearts without EADs. This increase in CaM kinase activity was prevented by pretreatment with KN-93. [1]
In vitro, KN-93 potently suppressed rabbit myocardial CaM kinase activity (calculated Ki ≤ 2.58 μM), but the inactive analog KN-92 did not (Ki > 100 μM). The actions of KN-93 and KN-92 on ICa and other repolarizing K+currents did not illustrate preferential EAD suppression by KN-93. [1]
Reference:
1. 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.
| Cell experiment[1]: | |
|
Cell lines |
NIH 3T3 fibroblasts |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
72 h, 4-24 μM |
|
Applications |
KN-92 is an inactive derivative of KN-93. KN-92 is usually used as a control in studies to elucidate the effect of KN-93. KN-93 inhibits fibroblast CaMK-II activity and cell growth, whereas KN-92 had no effect on CaMK-II activity or cell growth. |
| Animal experiment [2]: | |
|
Animal models |
AC3-I and AC3-C transgenic mice |
|
Dosage form |
20 μmol/kg, intraperitoneal |
|
Application |
Treatment with KN-93 in WT mice resulted in a dose-dependent improvement in left ventricular function compared to WT mice treated with KN-92. Surviving myocytes from infarcted wild-type mice without treatment or treated with control drug KN-92 exhibited severely disordered Ca2+ homeostasis. In contrast, Ca2+ homeostasis was preserved after myocardial infarction in wild-type mice treated with KN-93. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Tombes R M, Grant S, Westin E H, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK-II (the multifunctional Ca2+/CaM kinase)[J]. Cell growth & differentiation: the molecular biology journal of the American Association for Cancer Research, 1995, 6(9): 1063. [2]. Zhang R, Khoo M S C, Wu Y, et al. Calmodulin kinase II inhibition protects against structural heart disease[J]. Nature medicine, 2005, 11(4): 409-417. | |
| Cas No. | 1431698-47-3 | SDF | |
| Chemical Name | (E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide hydrochloride | ||
| Canonical SMILES | ClC1=CC=C(/C=C/CN(C)CC2=CC=CC=C2NS(C3=CC=C(OC)C=C3)(=O)=O)C=C1.Cl | ||
| Formula | C24H26Cl2N2O3S | M.Wt | 493.45 |
| Solubility | ≥ 24.65 mg/mL in DMSO, ≥ 11.73 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0265 mL | 10.1327 mL | 20.2655 mL |
| 5 mM | 0.4053 mL | 2.0265 mL | 4.0531 mL |
| 10 mM | 0.2027 mL | 1.0133 mL | 2.0265 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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