Merck, 420097-500UG, JAK Inhibitor I

General description
A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC₅₀ = 15 nM for murine JAK1), JAK2 IC₅₀ = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC₅₀ = 1 nM). It inhibits other kinases only at much higher concentrations. Also inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks the phosphorylation of STAT5.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
murine JAK1
Product competes with ATP.
Reversible: yes
Target IC₅₀: 15 nM, 1 nM against murine JAK1 and JAK2, respectively; 1 nM against Tyk2
Target Ki: 5 nM against JAK3
Packaging
Packaged under inert gas
Physical form
A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
Preparation Note
Following initial use, aliquot and refrigerate (4°C).
Other Notes
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)