1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. JAK3-IN-17

JAK3-IN-17 is an orally active JAK3 inhibitor (IC50: 14.56 nM). JAK3-IN-17 inhibits the production of IL-2 and IL-6 in a DNCB-induced mouse atopic dermatitis model and exhibits anti-inflammatory activity.

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JAK3-IN-17 Chemical Structure

JAK3-IN-17 Chemical Structure

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Description

JAK3-IN-17 is an orally active JAK3 inhibitor (IC50: 14.56 nM). JAK3-IN-17 inhibits the production of IL-2 and IL-6 in a DNCB-induced mouse atopic dermatitis model and exhibits anti-inflammatory activity[1].

IC50 & Target[1]

JAK3

14.56 nM (IC50)

Parmacokinetics[1]
Species Dose Route Indicator value
Rat 2 mg/kg i.v. T1/2 2.68 hr
Rat 20 mg/kg p.o. T1/2 20.33 hr
Rat 2 mg/kg i.v. Tmax 0.75 hr
Rat 20 mg/kg p.o. Tmax 0.5 hr
Rat 2 mg/kg i.v. Cmax 53.13 ng/mL
Rat 20 mg/kg p.o. Cmax 29.7 ng/mL
Rat 2 mg/kg i.v. AUC0-t 0.1042 μg·h/mL
Rat 20 mg/kg p.o. AUC0-t 0.9504 μg·h/mL
Rat 2 mg/kg i.v. AUC0-∞ 0.1053 μg·h/mL
Rat 20 mg/kg p.o. AUC0-∞ 0.2884 μg·h/mL
Rat 2 mg/kg i.v. MRT0-t 1.66 hr
Rat 20 mg/kg p.o. MRT0-t 4.42 hr
Rat 2 mg/kg i.v. MRT0-∞ 190.8 hr
Rat 20 mg/kg p.o. MRT0-∞ 27.77 hr
Rat 2 mg/kg i.v. CL 19.56 L/h/kg
Rat 20 mg/kg p.o. CL 123.87 L/h/kg
Rat 2 mg/kg i.v. F 27.38 %
Molecular Weight

358.37

Formula

C21H15FN4O

SMILES

O=C(C=C)NC1=CC=CC(C2=CN=C3C=CC(C4=C(F)N=CC=C4)=CN32)=C1

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
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JAK3-IN-17
Cat. No.:
HY-173601
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