.cp_wz tabla {borde superior: 1px sólido #ccc; borde izquierdo: 1px sólido #ccc; } .cp_wz table td {borde derecho: 1px sólido #ccc; borde inferior: 1px sólido #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; relleno: 5px 0px 0px 5px;} \ n Peso molecular: \ n 332.42 El inhibidor de JNK IX es un inhibidor de JNK selectivo y potente con pIC50 de 6.5 y 6.7 para JNK2 y JNK3, respectivamente. \ n Actividad biológica
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Description
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JNK inhibitor IX is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively.
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Targets
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JNK3 [1]
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JNK2 [1]
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IC50
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6.7(pIC50)
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6.5(pIC50)
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In vitro
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JNK inhibitor IX significantly reduces caspase-3 activity by the inhibition of JNK activity in human dermal fibroblasts. JNK inhibition by JNK inhibitor IX significantly increases apoptotic death in response to imatinib mesylate (IM) by preventing c-ABL complete de-phosphorylation at Ser residues.
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In vivo
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Features
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Protocolo (solo como referencia) Ensayo de quinasa: [1]
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JNK3 kinase inhibitory activity
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JNK3 kinase inhibitory activity is determined using a fluorescence anisotropy kinase binding assay. The kinase, a fluorescently labelled inhibitor and a variable concentration of test compound are incubated together to reach thermodynamic equilibrium under conditions such that in the absence of test compound the fluorescent inhibitor is significantly (>50%) enzyme bound and in the presence of a sufficient concentration of a potent inhibitor the anisotropy of the unbound fluorescent ligand is measurably different from the bound value. Truncated human JNK3 is expressed in baculovirus as a N-terminal His (6)-tagged fusion protein. This enzyme (JNK3) is activated in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 0.1 mM sodium vanadate, 10 mM magnesium acetate, 0.1 mM ATP with 100 nM active MKK4 and MKK7β at 30°C for 30 min. Following activation, the JNK3 is purified by Ni-NTA agarose chromatography. The JNK3 is then dialyzed into storage buffer (50 mM Tris/HCl, pH 7.5, 270 mM Sucrose, 150 mM NaCl, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 0.03% Brij-35, 1 mM benzamidine and 0.2 mM PMSF), snap frozen in liquid nitrogen and stored at −70°C. Inhibitor binding to JNK3 is assessed by a fluorescence anisotropy competitive binding assay. All components are dissolved in buffer of composition 50 mM Hepes, pH 7.5, 1 mM CHAPS, 1 mM DTT, 10 mM MgCl2 with final concentrations of 10 nM JNK3 and 2 nM of a fluorescently labelled inhibitor. This reaction mixture is added to wells containing various concentrations of test compound (0.28 nM-16.6 μM final) or DMSO vehicle (
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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Por ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de resveratrol de 11,2 mg / kg.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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Información química
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Molecular Weight (MW)
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332.42
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Formula
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C20 H16 N2 O S
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CAS No.
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312917-14-9
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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TCS JNK 5a
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Solubility (25°C) *
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In vitro
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DMSO
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20 mg/mL
(60.16 mM)
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Water
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<1 mg/mL
(
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Ethanol
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<1 mg/mL
(
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* <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.
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Chemical Name
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1-Naphthalenecarboxamide, N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)-
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : MAPK > Inhibidor de JNK
