Supplementary Materials

Supplementary Materials for:

Blockade of Glioma Proliferation Through Allosteric Inhibition of JAK2

Kunyan He, Qi Qi, Chi-Bun Chan, Ge Xiao, Xia Liu, Carol Tucker-Burden, Liya Wang, Hui Mao, Xiang Lu, Frank E. McDonald, Hongbo Luo, Qi-Wen Fan, William A. Weiss, Shi-Yong Sun, Daniel J. Brat, Keqiang Ye*

*Corresponding author. E-mail:

This PDF file includes:

  • Fig. S1. Effect of G5-7 derivatives (G5-X-2, -3, -5, -7, and -8) on the proliferation of U87MG/EGFRvIII and U87MG/PTEN cells.
  • Fig. S2. G5-7 reduces human GBM proliferation and viability in vitro.
  • Fig. S3. Effect of G5-7 on N09-24 and N08-30 neurospheres.
  • Fig. S4. Effect of G5-7 on the phosphorylation of Akt in U87MG isogenic cell lines.
  • Fig. S5. G5-7 does not directly block PTP1B, EGFR, and mTOR kinase activity.
  • Fig. S6. Confirmation of the binding of G5-7 and JAK2.
  • Fig. S7. Effect of gefitinib and ruxolitinib on the proliferation of U87MG/EGFRvIII and U87MG/PTNE cells.
  • Fig. S8. G5-7 blocks tumor growth of U87MG/EGFRvIII in subcutaneous model.
  • Fig. S9. Lestaurtinib inhibits U87MG/EGFRvIII tumor growth in subcutaneous model.
  • Fig. S10. Effect of the metabolite of G5-7 (M-G5-7) on phosphorylation of Akt and ERK in U87MG/EGFRvIII cells.
  • Fig. S11. Effect of G5-7 on VEGF mRNA abundance and JAK2-related signaling.
  • Fig. S12. Effect of G5-7 on GSH depletion and effect of G5-7 and G5-7-H on cell proliferation.
  • Fig. S13. Effect of hydrogen peroxide (H2O2) and Auranofin on signaling and apoptosis pathways in U87MG/EGFRvIII cells and on PTP1B activity in vitro.
  • Fig. S14. Effect of EKB-569 on GSH depletion in different kinds of cells.
  • Table S1. Chemical structures of G5-7 derivatives.
  • Table S2. Kinase profiling of G5-7.
  • Table S3. Complete blood count of vehicle- and G5-7–treated mice.

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Citation: K. He, Q. Qi, C.-B. Chan, G. Xiao, X. Liu, C. Tucker-Burden, L. Wang, H. Mao, X. Lu, F. E. McDonald, H. Luo, Q.-W. Fan, W. A. Weiss, S.-Y. Sun, D. J. Brat, K. Ye, Blockade of Glioma Proliferation Through Allosteric Inhibition of JAK2. Sci. Signal. 6, ra55 (2013).

© 2013 American Association for the Advancement of Science