1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. JAK3-IN-6

JAK3-IN-6 

Cat. No.: HY-101976
Handling Instructions

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

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

JAK3-IN-6 Chemical Structure

JAK3-IN-6 Chemical Structure

CAS No. : 1443235-95-7

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Description

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

IC50 & Target

JAK3

0.15 nM (IC50)

In Vitro

JAK3-IN-6 (compound 2), a potent inhibitor of JAK3 (0.15 nM) is 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). Irreversible JAK3-IN-6 with a JAK1 selective inhibitor 3 (JAK1: 0.96 nM, JAK2: 14 nM, JAK3: >1500 nM, TYK2: 10 nM) are cross titrated to determine if there is an additive or synergistic effect of co-inhibiting JAK1 and JAK3 enzymes on IL-7 signaling in CD3+, CD4+ PBMCs. As shown, the predicted levels of pSTAT5 inhibition based on addition of JAK1 and JAK3 inhibition are very close to the measured effects of cross titrating each compound, demonstrating that there is an additive effect but no synergistic effect of inhibiting JAK1 and JAK3 on blocking STAT5 phosphorylation. Furthermore inhibition of either JAK1 or JAK3 alone is sufficient to fully inhibit pSTAT5[2].

Storage

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

References
Molecular Weight

350.37

Formula

C₁₉H₁₈N₄O₃

CAS No.

1443235-95-7

SMILES

O=C(C1=CNC2=NC=NC(C3=CC=CC(NC(C(C)=C)=O)=C3)=C21)OCC

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Room temperature in continental US; may vary elsewhere

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Product Name:
JAK3-IN-6
Cat. No.:
HY-101976
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JAK3-IN-6

Cat. No.: HY-101976