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Cat. No.: 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 No.: 1644386-60-6
화학식: C₂₄H₁₈F₆N₆O₄S
분자량:600.49

보관:

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

Iso-AS601245 TFA Chemical Structure

CAS No.: 1644386-60-6

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

JNK1

0.15 μM (IC₅₀)

JNK2

0.22 μM (IC₅₀)

JNK3

0.07 μM (IC₅₀)

IL-2

All JNK Isoforms :

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

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 No. 1644386-60-6
분자량 600.49
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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수량:
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상품명:
CAS No.:
Species:
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Iso-AS601245 TFA

All JNK Isoforms

All TNF Receptor Isoforms

All Interleukin Related Isoforms