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Cat. No.: HY-133747

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JAK3-IN-9

JAK3-IN-9 is an orally active JAK3 inhibitor with IC₅₀ value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research.

For research use only. We do not sell to patients.

CAS No.: 1430095-30-9
Formula: C₁₇H₂₃N₅O₄S
Molecular Weight:393.46

Storage:

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

JAK3-IN-9 Chemical Structure

CAS No.: 1430095-30-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

JAK3

1.7 nM (IC₅₀)

All JAK Isoforms :

In Vitro

JAK3-IN-9 (compound 11i) shows high selective inhibition of JAK3 with IC₅₀ value of 1.7 nM ^[1].

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

Cell Viability Assay

Cell Line:

PBMCs^[1]
Concentration:

1 μM
Incubation Time:

30 min
Result:

Showed preferential inhibition of JAK3^[1].

In Vivo

JAK3-IN-9 (compound 11i) (Female Lewis rats; 3, 10 and 30 mg/kg; Oral gavage once daily for 20 days) can selectively inhibit JAK3 cytokine signaling in the primary cells^[1].
JAK3-IN-9 (Male DBA1j of 8 to 12-weeks old mice; 1mg/kg, Intravenous injection, Single administration) shows high AUC of 2104 μg/ml, extends t_1/2 to 2.56 h and good oral bioavailability of 48%^[1].
JAK3-IN-9 (30 mg/kg; Oral gavage once daily for 20 days) suppress paw swelling in a dose-dependent manner with ED₅₀ value of 10 mg/kg^[1].

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

Animal Model:

Male DBA1j (8 to 12-weeks old) mice; Female Lewis rats^[1].
Dosage:

1, 3, 10 and 30 mg/kg
Administration:

I.V, Single administration; IG, once daily for 20 days.
Result:

Showed anti-arthritis activity in the CIA mice model^[1].

Chemical Information

CAS No. 1430095-30-9
Molecular Weight 393.46
Formula C₁₇H₂₃N₅O₄S
SMILES

CC(C)[C@@H](C)NC1=C(C(N)=O)C=NC(NC2=CC=C(OS(=O)(C)=O)C=C2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bahekar R, et al. Discovery of diaminopyrimidine-carboxamide derivatives as JAK3 inhibitors. Bioorg Chem. 2020 Jun;99:103851. [Content Brief]

Calculators

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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.

Keywords

100 mg

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