| Bioactivity | FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM. | ||||||||||||
| Invitro | DLBCL cells are exposed to 50 μM FX1 for 30 minutes. FX1 profoundly reduces recruitment of BCOR and SMRT to all 3 BCL6 target genes, but not at a negative control locus. There is little presence of SMRT at these loci in the BCL6-negative DLBCL cell line, which is not affected by FX1. The superior potency of FX1 versus 79-6 in disrupting BCL6 binding to SMRT is evident when these small molecules are compared head to head in quantitative ChIP assays in DLBCL cells after treatment with 50 μM FX1 for 6 hours. DLBCL cells are exposed to FX1 and mRNA is collect at 4 serial time points. FX1 almost invariantly induces significant derepression of these genes as compare with vehicle in 2 independent DLBCL cell lines[1]. | ||||||||||||
| Name | FX1 | ||||||||||||
| CAS | 1426138-42-2 | ||||||||||||
| Formula | C14H9ClN2O4S2 | ||||||||||||
| Molar Mass | 368.82 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|