ZM39923

ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.

Research Areas >> Cancer

Research Areas >> Neurological Disease

JAK3:7.1 (pIC50)

JAK1:4.4 (pIC50)

EGF-R:5.6 (pIC50)

Lck:5.0 (pIC50)

CDK4:5.0 (pIC50)

TGM2:10 nM (IC50)

ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1. ZM39923 (Compound 7) shows weak inhibitory effect on EGF-R and JAK1 (pIC50, 5.6, 4.4, respectively), and insignificantly inhibits tyrosine kinases Lck and CDK4 (pIC50 <5.0)[1]. ZM39923 potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM, and acts directly on purified TGM2 to inhibit the Ca2+ activated form of TGM2[2]. ZM39923 blocks the phosphorylation of JAK3 induced by CCL19, and such an effect is similar to that of CCR7 antibody. ZM39923 also significantly blocks the CCL19 induced wound closure rate, and decreases the migration and invasion of PCI-37B cells[3].

PCI-37B (a metastatic SCCHN cell line expressing CCR7) cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum, penicillin, and streptomycin in an atmosphere of 5% CO2 and 95% air at 37°C. The ZM39923 inhibitor treatment at the dose determined using the Cell Counting Kit-8[3].

[1]. Brown GR, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9.

[2]. Lai TS, et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008 Sep 22;15(9):969-78.

[3]. Zhang Z, et al. Jak3 is involved in CCR7-dependent migration and invasion in metastatic squamous cell carcinoma of the head and neck. Oncol Lett. 2017 May;13(5):3191-3197.

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