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Purity: ≥98%
FX1 is a potent and specific inhibitor of the BCL6 (B cell lymphoma 6) with an IC50 of approximately 35 μM. FX1 is ten times more powerful than the endogenous corepressors and binds to a crucial portion of the BCL6 lateral groove. FX1 mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations and disrupted the formation of the BCL6 repression complex, reactivating BCL6 target genes. In mice with DLBCL xenografts, low doses of FX1 caused the regression of tumors that had already developed. In addition, ex vivo primary human ABC-DLBCL specimens as well as ABC-DLBCL cells grown in vitro and in vivo were suppressed by FX1. All three of the BCL6 target genes are markedly reduced in BCOR and SMRT recruitment by FX1, but not at a negative control locus.
| Targets |
BCL6 (IC50 ~35 μM)
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| ln Vitro |
For 30 minutes, DLBCL cells are exposed to 50 μM FX1. All three of the BCL6 target genes are markedly reduced in BCOR and SMRT recruitment by FX1, but not at a negative control locus. The BCL6-negative DLBCL cell line, which is unaffected by FX1, has little SMRT at these loci. When FX1 and 79-6 are pitted against one another in quantitative ChIP assays in DLBCL cells after treatment with 50 μM FX1 for 6 hours, it is clear that FX1 has greater potency than 79-6 in preventing BCL6 binding to SMRT. mRNA is collected at four sequential time points after FX1 exposure to DLBCL cells. In two separate DLBCL cell lines, FX1 almost always significantly induces derepression of these genes when compared with vehicle[1].
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| ln Vivo |
Spleens in FX1-treating mice are macroscopically indistinguishable from vehicle controls. TFX1 has no impact on the overall abundance of B cells as determined by flow cytometry. When exposed to FX1, GC B cells (GL7+FAS+B220+) are significantly reduced. IHC analyzes the architecture of the spleen. Normal B cell follicular structures can be seen after staining with the B220 antibody, but a significant loss of GCs can be seen after staining with the GC-specific B cell marker peanut agglutinin. The half-life is thought to be 12 hours or so. Finally, it is determined if FX1 can cause toxic effects in mice. H&E-stained sections of the lung, digestive tract, heart, kidney, liver, spleen, and bone marrow of mice treated with FX1 compared with vehicle show no signs of toxicity, inflammation, or infection[1].
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| Cell Assay |
Using antibodies for BCL6, SMRT, BCOR, or IgG control, quantitative ChIP is carried out in SUDHL-6 cells exposed to FX1 (black bars) or vehicle (white bars) in DLBCL cells in order to enrich for known BCL6 binding sites in the CD69, CXCR4, and DUSP5 loci, as well as a negative control region.
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| Animal Protocol |
SCID mice bearing SUDHL-6 xenografts
50 mg/kg i.p. |
| References |
| Molecular Formula |
C14H9CLN2O4S2
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| Molecular Weight |
368.82
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| Exact Mass |
367.969
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| Elemental Analysis |
C, 45.59; H, 2.46; Cl, 9.61; N, 7.60; O, 17.35; S, 17.39
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| CAS # |
1426138-42-2
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| Appearance |
Red solid powder
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| SMILES |
C1=CC2=NC(=O)C(=C2C=C1Cl)C3=C(N(C(=S)S3)CCC(=O)O)O
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| InChi Key |
JYBGCTWNOMSQJY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9ClN2O4S2/c15-6-1-2-8-7(5-6)10(12(20)16-8)11-13(21)17(14(22)23-11)4-3-9(18)19/h1-2,5,21H,3-4H2,(H,18,19)
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| Chemical Name |
3-[5-(5-chloro-2-oxoindol-3-yl)-4-hydroxy-2-sulfanylidene-1,3-thiazol-3-yl]propanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7113 mL | 13.5567 mL | 27.1135 mL | |
| 5 mM | 0.5423 mL | 2.7113 mL | 5.4227 mL | |
| 10 mM | 0.2711 mL | 1.3557 mL | 2.7113 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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