KN-93

Catalog No.S6787 Batch:S678702

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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 50 mg/mL (99.79 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
5% DMSO 95% Corn oil
1.65mg/ml
* <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.)

Preparing Stock Solutions

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.

Selleck's KN-93 has been cited by 32 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
In vitro and in vivo inhibition of the host TRPC4 channel attenuates Zika virus infection [ EMBO Mol Med, 2024, 10.1038/s44321-024-00103-4] PubMed: 39009885
CaMKII suppresses proteotoxicity by phosphorylating BAG3 in response to proteasomal dysfunction [ EMBO Rep, 2024, 25(10):4488-4514] PubMed: 39261742
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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