1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Metabolic Enzyme/Protease
  2. JAK Tyrosinase
  3. JAK3-IN-18

JAK3-IN-18 is an orally active JAK3 and TEC inhibitor, with IC50s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis.

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

JAK3-IN-18 Chemical Structure

JAK3-IN-18 Chemical Structure

CAS No. : 2914873-59-7

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Description

JAK3-IN-18 is an orally active JAK3 and TEC inhibitor, with IC50s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis[1].

IC50 & Target[1]

JAK3

0.5391 nM (IC50)

JAK1

8575 nM (IC50)

JAK2

7431 nM (IC50)

In Vitro

JAK3-IN-18 (Compound 8a) (1-100000 nM, 80 min) inhibits p-stat5 with an IC50 value of 177.8 nM in the IL-15-stimulated human whole blood (HWB) assay[1].
JAK3-IN-18 (1 μM, 135 min) inhibits only 11 kinases with more than 60% inhibition apart from JAK3 and TEC against 310 kinases[1].
JAK3-IN-18 (10 μM, 0-60 min) exhibits acceptable GSH stability with favorable drug-like properties[1].

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

In Vivo

JAK3-IN-18 (Compound 8a) (10-100 mg/kg, p.o., twice daily, 24 days ) demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis[1].

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

Animal Model: Experimental autoimmune encephalomyelitis (EAE) mice (6-8 weeks)[1]
Dosage: 10, 100 mg/kg
Administration: p.o. twice daily for 24 days
Result: Decreased the clinical scores.
Showed no body weight loss.
Molecular Weight

337.35

Formula

C18H16FN5O

CAS No.
SMILES

O=C(C=C)N1CC2=C([C@@H](NC3=C4C=CNC4=NC=N3)C1)C=CC(F)=C2

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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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  • 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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JAK3-IN-18
Cat. No.:
HY-174999
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