Home Apoptosis Bcl-6 inhibitor - Apoptosis related activator FX1 For research use only.

FX1

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. FX1 induces apoptosis.

FX1 Chemical Structure

FX1 Chemical Structure

CAS No. 1426138-42-2

Purity & Quality Control

FX1 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TMD8 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human TMD8 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM. 28485934
SUDHL4 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human SUDHL4 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM. 28485934
OCI-LY19 Antiproliferative assay 3 days Antiproliferative activity against BCL6 independent human OCI-LY19 cells after 3 days by CellTiter-Glo assay, GI50 = 10 μM. 28485934
OCI-LY10 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human OCI-LY10 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM. 28485934
SU-DHL-2 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human SU-DHL-2 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM. 28485934
U2932 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human U2932 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM. 28485934
KARPAS422 Antiproliferative assay 3 days Antiproliferative activity against BCL6 independent human KARPAS422 cells after 3 days by CellTiter-Glo assay, GI50 = 12.5892 μM. 28485934
OCI-LY1 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human OCI-LY1 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM. 28485934
OCI-LY3 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human OCI-LY3 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM. 28485934
AMO1 Antiproliferative assay 3 days Antiproliferative activity against BCL6 dependent human AMO1 cells after 3 days by CellTiter-Glo assay, GI50 = 19.9526 μM. 28485934
Click to View More Cell Line Experimental Data

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. FX1 induces apoptosis.
Features Recommend for freshly prepared each time for in vitro experiment
Targets
BCL6 BTB [1]
(Cell-free assay)
35 μM
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models SCID mice bearing SUDHL-6 xenografts
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02902679 Completed
Thrombosis|Factor XI|Renal Impairment|ESRD (End-Stage Renal Disease)
Bristol-Myers Squibb
 November 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 368.82 Formula

C14H9ClN2O4S2
CAS No. 1426138-42-2 SDF Download FX1 SDF
Smiles C1=CC2=NC(=O)C(=C2C=C1Cl)C3=C(N(C(=S)S3)CCC(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (54.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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