Supplementary Materials

This PDF file includes:

  • Fig. S1. AMD3100 increases CXCR4 abundance in Jurkat cells.
  • Fig. S2. Neither AMD3100 nor X4-2-6 causes CXCR4 internalization.
  • Fig. S3. AMD3100 but not X4-2-6 inhibits CXCL12-stimulated CXCR4 endocytosis.
  • Fig. S4. BA2 recruitment downstream of CXCR4 is not substantially affected by X4-2-6.
  • Fig. S5. X4-2-6 does not inhibit BA2 recruitment to CXCR4.
  • Fig. S6. BA1/2 regulates ERK phosphorylation downstream of CXCR4.
  • Fig. S7. CXCR4 and CCR2 share 63% amino acid sequence similarity in the region of the receptor corresponding to X4-2-6.
  • Fig. S8. X4-2-6 inhibits the CXCL12-mediated chemotaxis of THP-1 cells.
  • Fig. S9. X4-2-6 binds directly to CXCL12.
  • Fig. S10. AMD3100 displaces the N terminus of CXCL12 from the binding site of CXCR4.
  • Fig. S11. The small molecule SEN071 is a biased antagonist of CXCR4 that avoids antagonist tolerance.

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