FX1

Catalog No.S8591

FX1 Chemical Structure

Molecular Weight(MW): 368.82

FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases.

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Biological Activity

Description FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases.
Targets
BCL6 BTB [1]
(Cell-free assay)
35 μM
In vitro

FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo. FX1 is specific to BCL6 and binds with a greater affinity than the natural BCL6 ligand SMRT. FX1 almost invariantly induced significant derepression of these genes(BCL6 target genes CASP8, CD69, CXCR4, CDKN1A, and DUSP5) as compared with vehicle in 2 independent DLBCL cell lines. FX1 was more than 100-fold more powerful than the previous generation of BCL6 inhibitors represented by 79-6, and 300-fold more potent than the recently reported binding of the antibiotics rifamycin and rifabutin (KD ~1 mM)[1].

In vivo Low doses of FX1 induce regression of established tumors in mice bearing DLBCL xenografts. The half-life is estimated to be approximately 12 hours for FX1 in SCID mice. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of lung, gastrointestinal tract, heart, kidney, liver, spleen, and bone marrow of the fixed organs from mice treated with FX1 compared with vehicle. Peripheral blood counts and serum chemistry in FX1-treated mice are also examined and they remain within normal parameters. FX1 causes profound and significant suppression of DLBCLs in DLBCL xenografts, and indeed not only prevented growth of the xenografts but in addition causes these tumors to shrink from their initial volume. The maximal effect is already achieved by the lower 25 mg/kg dose. TUNEL and Ki-67 staining shows that FX1 also induced more apoptosis and growth arrest than 79-6, respectively[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: DLBCL cells, SUDHL-6 cells
  • Concentrations: 50 μM
  • Incubation Time: 30 min
  • Method:

    Quantitative ChIP is performed in SUDHL-6 cells exposed to FX1 (black bars) or vehicle (white bars) in DLBCL cells using antibodies for BCL6, SMRT, BCOR, or IgG control to enrich for known BCL6 binding sites in the CD69, CXCR4, and DUSP5 loci, or a negative control region.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: SCID mice bearing SUDHL-6 xenografts
  • Formulation: 35% PEG-300, 5% Tween-80, 65% Dextrose 5%
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.92 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 368.82
Formula

C14H9ClN2O4S2

CAS No. 1426138-42-2
Storage powder
Synonyms N/A

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID