KN-93

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.

KN-93 Chemical Structure

KN-93 Chemical Structure

CAS No. 139298-40-1

Purity & Quality Control

KN-93 Related Products

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
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]

Cell Research 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.

In Vivo
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]

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

Chemical Information & Solubility

Molecular Weight 501.04 Formula

C26H29ClN2O4S

CAS No. 139298-40-1 SDF --
Smiles CN(CC=CC1=CC=C(C=C1)Cl)CC2=CC=CC=C2N(CCO)S(=O)(=O)C3=CC=C(C=C3)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (199.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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