INSOLUTION JAK INHIBITOR I - CAS 457081-03-7 - CALBIOCHEM

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 (K_i = 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 K_i: 5 nM against JAK3

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.

Reconstitution

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

Molecular Weight: 309.34. Empirical Formula: C₁₈H₁₆FN₃O. Quality Level: 100. Assay: ≥. 98% (HPLC). form: liquid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. shipped in: wet ice. storage temp.: 2-8°C. InChI: 1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22). InChI key: VNDWQCSOSCCWIP-UHFFFAOYSA-N. Storage Class Code: 10 - Combustible liquids. WGK: WGK 2. Flash Point(F): 188.6 °F - (Dimethylsulfoxide). Flash Point(C): 87 °C - (Dimethylsulfoxide).