KN-93

Catalog No.S6787 Batch:S678701

Technical Data

Formula	C₂₆H₂₉ClN₂O₄S
Molecular Weight	501.04	CAS No.	139298-40-1
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (199.58 mM)
		Ethanol	21 mg/mL (41.91 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

KN-93 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity.

Targets

CaMKII ^[1]
(Cell-free assay)

2.58 μM(Ki)

In vitro

KN-93, a CaMK2 inhibitor, reduces the B-cell differentiation and IgG production by differentiated plasma cells, and inhibits Blimp-1 expression in B cells.^[2]

In vivo

KN93 shows the protective effect on acute pancreatitis (AP) at a dose-dependent way, with no toxic side effects on the mice.^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines human B cells isolated from lupus nephritis (LN) patients Concentrations 5 μM Incubation Time -- Method For B-cell differentiation, isolated naive B cells were cultured in Roswell Park Memorial Institute (RPMI) 1640 supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were stimulated with antihuman IgM (5 μg/ml) and antihuman CD40 (1 μg/ml) antibodies in the presence of interleukin (IL)-2 (20 ng/ml), IL-4 (25 ng/ml) and IL-21 (50 ng/ml) for 8 days. For signaling study, cells treated with KN-93 (1 μM) to study the roles of CaMK2 in human B-cell differentiation. Proteins were loaded to sodium dodecyl sulfate (SDS)-polyacrylamide gels and electrotransferred onto polyvinylidine difluoride membranes after separation. Membranes were blocked with 5% bovine serum albumin in TBST buffer and incubated with primary antibodies against ORAI1, ORAI2, STIM2, Blimp-1, and p-CaMK2, at 4°C overnight. Membranes were incubated with anti-GAPDH primary antibody and used as internal control. Membranes were then washed with TBST and incubated with horseradish-peroxidase-conjugated antirabbit or antimouse IgG at room temperature for 60 min. Signals were detected by enhanced chemiluminescence analysis kit.
Animal Study:^{^[3]}	Animal Models mice of acute pancreatitis (AP) model Dosages 5, 10, 20 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
human B cells isolated from lupus nephritis (LN) patients
Concentrations
5 μM
Incubation Time
--
Method
For B-cell differentiation, isolated naive B cells were cultured in Roswell Park Memorial Institute (RPMI) 1640 supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were stimulated with antihuman IgM (5 μg/ml) and antihuman CD40 (1 μg/ml) antibodies in the presence of interleukin (IL)-2 (20 ng/ml), IL-4 (25 ng/ml) and IL-21 (50 ng/ml) for 8 days. For signaling study, cells treated with KN-93 (1 μM) to study the roles of CaMK2 in human B-cell differentiation. Proteins were loaded to sodium dodecyl sulfate (SDS)-polyacrylamide gels and electrotransferred onto polyvinylidine difluoride membranes after separation. Membranes were blocked with 5% bovine serum albumin in TBST buffer and incubated with primary antibodies against ORAI1, ORAI2, STIM2, Blimp-1, and p-CaMK2, at 4°C overnight. Membranes were incubated with anti-GAPDH primary antibody and used as internal control. Membranes were then washed with TBST and incubated with horseradish-peroxidase-conjugated antirabbit or antimouse IgG at room temperature for 60 min. Signals were detected by enhanced chemiluminescence analysis kit.

Animal Study:^{^[3]}

Animal Models
mice of acute pancreatitis (AP) model
Dosages
5, 10, 20 mg/kg
Administration
i.p.

References

Selleck's KN-93 has been cited by 29 publications

CaMK4 controls follicular helper T cell expansion and function during normal and autoimmune T-dependent B cell responses [ Nat Commun, 2024, 15(1):840]	PubMed: 38287012
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300]	PubMed: 38346942
CaMKII regulates the proteins TPM1 and MYOM2 and promotes diacetylmorphine-induced abnormal cardiac rhythms [ Sci Rep, 2023, 13(1):5827]	PubMed: 37037889
Late sodium current in synergism with Ca2+/calmodulin-dependent protein kinase II contributes to β-adrenergic activation-induced atrial fibrillation [ Philos Trans R Soc Lond B Biol Sci, 2023, 378(1879):20220163]	PubMed: 37122215
SGLT2 inhibitor dapagliflozin reduces endothelial dysfunction and microvascular damage during cardiac ischemia/reperfusion injury through normalizing the XO-SERCA2-CaMKII-coffilin pathways [ Theranostics, 2022, 12(11):5034-5050]	PubMed: 35836807
Silica nanoparticles induce cardiac injury and dysfunction via ROS/Ca2+/CaMKII signaling [ Sci Total Environ, 2022, 837:155733]	PubMed: 35526619
Activation of transient receptor potential vanilloid 4 is involved in pressure overload-induced cardiac hypertrophy [ Elife, 2022, 11e74519]	PubMed: 35731090
Ion channel Piezo1 activation promotes aerobic glycolysis in macrophages [ Front Immunol, 2022, 13:976482]	PubMed: 36119083
Effects and potential mechanism of Ca2+/calmodulin‑dependent protein kinase II pathway inhibitor KN93 on the development of ovarian follicle [ Int J Mol Med, 2022, 50(4)121]	PubMed: 35929517
Effect of feeding regimen on circadian activity rhythms of food anticipatory by ghrelin hormone in a pig model [ Nutr Neurosci, 2022, 1-19]	PubMed: 35249475

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