KN-93

N.º de catálogoS6787 Lote:S678701

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Datos técnicos

Fórmula

C₂₆H₂₉ClN₂O₄S

Peso molecular

501.04

Número CAS

139298-40-1

Solubilidad (25°C)*

In vitro

DMSO

100 mg/mL (199.58 mM)

Ethanol

21 mg/mL (41.91 mM)

Water

Insoluble

In vivo (Agregue los solventes al producto individualmente y en orden.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción

KN-93 es un inhibidor permeable a las células, reversible y competitivo de la proteína quinasa II dependiente de Ca2+/calmodulina (CaMK-II) con un Ki de 2,58 μM en la actividad de la CaM quinasa miocárdica de conejo.

Objetivos

CaMKII
(Cell-free assay)

2.58 μM(Ki)

In vitro

KN-93, un inhibidor de CaMK2, reduce la diferenciación de células B y la producción de IgG por células plasmáticas diferenciadas, e inhibe la expresión de Blimp-1 en células B.

In vivo

KN93 muestra un efecto protector sobre la pancreatitis aguda (PA) de forma dosis-dependiente, sin efectos secundarios tóxicos en los ratones.

Protocolo (de referencia)

Ensayo celular:^{^[2]}	Líneas celulares human B cells isolated from lupus nephritis (LN) patients Concentraciones 5 μM Tiempo de incubación -- Método 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.
Estudio en animales:^{^[3]}	Modelos animales mice of acute pancreatitis (AP) model Dosificaciones 5, 10, 20 mg/kg Administración i.p.

Ensayo celular:^{^[2]}

Líneas celulares
human B cells isolated from lupus nephritis (LN) patients
Concentraciones
5 μM
Tiempo de incubación
--
Método
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.

Estudio en animales:^{^[3]}

Modelos animales
mice of acute pancreatitis (AP) model
Dosificaciones
5, 10, 20 mg/kg
Administración
i.p.

Referencias

https://pubmed.ncbi.nlm.nih.gov/9864285/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8569388/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8612788/

Sellecks KN-93 Ha sido citado por 35 Publicaciones

TRPA1 exacerbates selective retinal ganglion cell vulnerability under acute ocular hypertension [ Acta Neuropathol Commun, 2025, 13(1):70]	PubMed: 40186313
Mechanosensor Piezo1‑mediated smooth muscular cell pyroptosis contributes to vascular calcification [ Int J Mol Med, 2025, 56(5)196]	PubMed: 40937566
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
The Role of Sodium Fluoride Mouthwash in Regulating FGF-2 and TGF-β Expression in Human Gingival Fibroblasts [ Biomedicines, 2024, 12(8)1727]	PubMed: 39200192
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

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