1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

JAK-IN-1 

Cat. No.: HY-13827
Handling Instructions

JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.

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

JAK-IN-1 Chemical Structure

JAK-IN-1 Chemical Structure

CAS No. : 1334673-53-8

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.

IC50 & Target

IC50: 0.26 nM (JAK1), 0.8 nM (JAK2), 3.2 nM (JAK3)[1]

In Vitro

JAK-IN-1 inhibits the proliferation of human CD4 and CD8 T cells in a dose-dependent manner upon stimulation by anti-CD3/anti-CD28 antibody-coated beads partially mimicking the activation signals brought to a Tcell by an antigen-presenting cell. JAK-IN-1 is active in both mechanistic and functional cell-based assays using T-cells, one of the major cell types in which JAK3 is potentially relevant[1].

In Vivo

JAK-IN-1 is JAK3 selective in vivo, as judged by higher potency inhibiting JAK1/JAK3- vs JAK2- or JAK1/JAK2/TYK2-driven signaling in whole blood assays. JAK-IN-1 potently inhibits IL-2 stimulated plasma concentrations of JAK-IN-1 for each dose. JAK-IN-1 prevents IL-2-driven STAT5 phosphorylation in a dose- and concentration-dependent manner, with approximately 50% inhibition observed at the 10 mg/kg dose (plasma concentration ∼480 nM)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6285 mL 13.1427 mL 26.2854 mL
5 mM 0.5257 mL 2.6285 mL 5.2571 mL
10 mM 0.2629 mL 1.3143 mL 2.6285 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Carboxyfluorescein succinimidyl ester (CFSE)-labeled human PBMCs were exposed to JAK-IN-1 prior to stimulation with anti-CD3/anti-CD28 antibodies. Cell proliferation was then measured by CFSE dilutions as detected by flow cytometry in CD4 positive and CD8 positive T cells after staining with fluorochrome-conjugated antibodies[1]

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

Animal Administration
[1]

Mice[1]

Adult (10−12 weeks old) C57BL/6 mice are treated with JAK-IN-1 (0.3, 1, 3, 10, 30, and 100 mg/kg). Mice received a single oral suspension dose of JAK-IN-1 or vehicle alone. Two hours after treatment by oral gavage, mice were euthanized for collecting whole blood in heparinized tubes[1].

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

References
Molecular Weight

380.44

Formula

C₂₀H₂₄N₆O₂

CAS No.

1334673-53-8

SMILES

O=C(C1=CNC2=NC=C(C3CC3)N=C21)N[[email protected]@H](C(N4CC(C#N)C4)=O)C(C)(C)C

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
JAK-IN-1
Cat. No.:
HY-13827
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JAK-IN-1

Cat. No.: HY-13827