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KN-93

Catalog No. T2697 CAS 139298-40-1

KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.

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KN-93, CAS 139298-40-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 52.00
2 mg	In stock	$ 72.00
5 mg	In stock	$ 115.00
10 mg	In stock	$ 157.00
25 mg	In stock	$ 322.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 582.00
1 mL * 10 mM (in DMSO)	In stock	$ 129.00

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Purity: 99.86%

Purity: 99.78%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.
Targets&IC50	CaMK II:370 nM. (Ki)
In vitro	Following 2 days of treatment with KN-93, 95% of cells are halted in the G1 phase, a process which is reversible; one day post KN-93 withdrawal, a notable number of cells transition into the S and G2-M phases. KN-93 effectively inhibits cell growth prompted by various growth factors, including basic fibroblast growth factor, platelet-derived growth factor-BB, epidermal growth factor, and insulin-like growth factor-1, in NIH 3T3 fibroblasts[1]. Moreover, KN-93 disrupts H+, K+-ATPase activity, significantly dissipates the proton gradient across gastric membrane vesicles, and diminishes the luminal space volume[2]. At a concentration of 0.5 μM, KN-93 averts the increase in left ventricular (LV) developed pressure and the occurrence of early afterdepolarizations. It also blocks the rise in Ca2+-independent CaM kinase activity observed during these afterdepolarizations[3]. At a 10 μM concentration, KN-93 significantly suppresses the activation of CaMKII/NF-κB signaling triggered by high glucose levels, leading to a decreased expression of VEGF, iNOS, and ICAM-1 in Müller cells[4].
In vivo	KN-93, administered intraperitoneally at a dosage of 1 mg/kg/day, effectively reduces retinal vascular leakage in diabetes and concurrently inhibits the phosphorylation of CaMKII and NF-κB within the diabetic retina[4].
Kinase Assay	Cells are grown on 12-mm diameter glass coverslips in DMEM 100% serum and various concentrations of KN-93 or KN-92. After 0, 1, 2, and 3 days of culture in the presence of drug, coverslips are removed from culture, rinsed once in PBS, and then submerged in 100% methanol at -20°C for 3 min. Fixed cells are stored in PBS until staining using the TUNEL assay. Cells are overlaid on 20 μL PBS/1 mg/mL BSA for 30 min, rinsed in PBS, and then overlaid on 20 μL containing 100 mM sodium cacodylate (pH 6.8), 1 mM CoCl2, 0.1 mM DTT, 0.1 mg/mL BSA, 20 μM fluorescein-12-dUTP, and 0.1 unit/μL terminal transferase at 37°C for 60 min. Coverslips are rinsed in PBS twice, mounted on slides, and photographed using an OLYMPUS BX5O epifluorescent microscope using a UPLAN APO 40X oil immersion objective.
Cell Research	KN-93 is dissolved in DMSO. Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150 μL DMSO. The optical density of the solution is measured at 490 nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group).

Molecular Weight	501.04
Formula	C26H29ClN2O4S
CAS No.	139298-40-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: >10 mM

References and Literature

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. 5. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1[J]. Frontiers in Pharmacology. 2021, 11: 2233. 6. Xuexian Fang, Hao Wang, Dan Han, Enjun Xie, Xiang Yang, Jiayu Wei, Shanshan Gu et al. Ferroptosis as a target for protection against cardiomyopathy [J]. Proceedings of the National Academy of Sciences of the United States of America . 2019 Feb 12;116(7):2672-2680.

Citations

1. Xuexian Fang, Hao Wang, Dan Han, Enjun Xie, Xiang Yang, Jiayu Wei, Shanshan Gu et al. Ferroptosis as a target for protection against cardiomyopathy. Proceedings of the National Academy of Sciences of the United States of America. 2019 Feb 12;116(7):2672-2680. 2. Zheng Q, Zou Y, Teng P, et al. Mechanosensitive Channel PIEZO1 Senses Shear Force to Induce KLF2/4 Expression via CaMKII/MEKK3/ERK5 Axis in Endothelial Cells. Cells. 2022, 11(14): 2191 3. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1. Frontiers in Pharmacology. 2021 Jan 13;11:539261. doi: 10.3389/fphar.2020.539261. eCollection 2020. 4. Jiang Q, Li Y, Mao R, et al.AaCaMKs Positively Regulate Development, Infection Structure Differentiation and Pathogenicity in Alternaria alternata, Causal Agent of Pear Black Spot.International Journal of Molecular Sciences.2023, 24(2): 1381. 5. Yin Z, Zhang J, Zhao M, et al.Maresin‐1 ameliorates hypertensive vascular remodeling through its receptor LGR6.MedComm.2024, 5(3): e491.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Neuronal Signaling Compound Library Bioactive Lipid Compound Library Bioactive Compound Library Autophagy Compound Library

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Keywords

KN-93 139298-40-1 Autophagy Neuroscience CaMK Inhibitor KN93 Calmodulin-dependent protein kinases Calmodulin-dependent kinases inhibit KN 93 inhibitor

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