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Art. -Nr.: HY-10612A

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Iso-AS601245 TFA

Iso-AS601245 TFA is an orally active JNK inhibitor, with IC₅₀ values of 0.15 μM, 0.22 μM and 0.07 μM against JNK1, JNK2 and JNK3, respectively. Iso-AS601245 TFA reduces plasma TNF-α levels in mice and inhibits IL-2 secretion in activated T cells. Iso-AS601245 TFA alleviates adjuvant-induced rheumatoid arthritis in mice. Iso-AS601245 TFA can be used in studies related to rheumatoid arthritis.

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CAS. Nr.: 1644386-60-6
Formel: C₂₄H₁₈F₆N₆O₄S
Molecular Weight:600.49

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Iso-AS601245 TFA Chemical Structure

CAS. Nr.: 1644386-60-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

JNK1

0.15 μM (IC₅₀)

JNK2

0.22 μM (IC₅₀)

JNK3

0.07 μM (IC₅₀)

IL-2

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

In Vitro

Iso-AS601245 (Compound 59) (10 μM; 24.5 h) TFA inhibits IL-2 secretion by PMA (HY-18739)- and Ionomycin (HY-13434)-stimulated Jurkat human T lymphoblasts by 90% at a concentration of 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ELISA Assay^[1]

Cell Line:

Jurkat human T lymphoblast cell line
Concentration:

10 μM
Incubation Time:

30-minute pre-incubation; 24-hour stimulation/incubation
Result:

Inhibited IL-2 secretion by PMA and ionomycin-stimulated Jurkat cells by 90%.
Showed no observed cell toxicity at 10 μM.

In Vivo

Iso-AS601245 (Compound 59) (0.3-30 mg/kg; p.o.; single dose) TFA dose-dependently inhibits LPS (HY-D1056)-induced TNF-α release in mice with an ED₅₀ of 3 mg/kg via oral administration^[1].
Iso-AS601245 (60 mg/kg; p.o.; daily; 7 days) TFA significantly reduces paw swelling, clinical scores, cartilage erosion, and synovium inflammation in a mouse model of collagen-induced arthritis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C3H/HEN mice (8-week-old)^[1]
Dosage:

0.3 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose
Result:

Caused a dose-dependent decrease in plasma TNF-α levels.
Achieved an ED₅₀ of 3 mg/kg.

Animal Model:

DBA/1 mice (8-12-week-old, male)^[1]
Dosage:

20 mg/kg; 60 mg/kg
Administration:

p.o.; daily; 7 days
Result:

Elicited significant depression of paw swelling at 60 mg/kg.
Reduced total clinical score at 60 mg/kg.
Revealed significant preservation of joint areas (reduced cartilage erosion) and reduced synovium inflammation at 60 mg/kg.

Chemical Information

CAS. Nr. 1644386-60-6
Molecular Weight 600.49
Formel C₂₄H₁₈F₆N₆O₄S
SMILES

OC(C(F)(F)F)=O.N#C/C(C1=NC(NCCC2=CN=CC=C2)=NC=C1)=C3NC4=CC=CC=C4S/3.OC(C(F)(F)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Gaillard P, et al. Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. Journal of medicinal chemistry. 2005 Jul 14;48(14):4596-607. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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Iso-AS601245 TFA

Alle JNK Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen