FX1
Based on 2 publication(s) in Google Scholar
FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1426138-42-2
- Formula: C14H9ClN2O4S2
- Molecular Weight:368.82
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) FX1
More
Biological Activity
IC50: ~35 μM (BCL6)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| DOHH-2 | IC50 |
35.1 μM
Compound: 2; FX1
|
Antiproliferative activity against human DOHH2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human DOHH2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| Farage | IC50 |
33.9 μM
Compound: 2; FX1
|
Antiproliferative activity against human Farage cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Farage cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| L02 | IC50 |
>100 μM
Compound: 2; FX1
|
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| NCM460 | IC50 |
>100 μM
Compound: 2; FX1
|
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| OCI-Ly7 | IC50 |
39 μM
Compound: 2; FX1
|
Antiproliferative activity against human OCI-LY7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human OCI-LY7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| PNT1A | IC50 |
>100 μM
Compound: 2; FX1
|
Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| SUD4 | IC50 |
51.3 μM
Compound: 2; FX1
|
Antiproliferative activity against human SUDHL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human SUDHL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
| Toledo | IC50 |
65.3 μM
Compound: 2; FX1
|
Antiproliferative activity against BCL6-negative human Toledo cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against BCL6-negative human Toledo cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 31895575] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1426138-42-2
-
Appearance Solid
-
Molecular Weight 368.82
-
Formula C14H9ClN2O4S2
-
Color Pink to red
-
SMILES
O=C(O)CCN(C/1=O)C(SC1=C2C(NC3=C/2C=C(Cl)C=C3)=O)=S
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Cell Rep
Loss of p53 exacerbates autoimmunity by reprogramming propionyl-CoA metabolism and histone modifications in Treg cells. [Abstract]2026 Mar 15;45(3):117084. PMID: 41838722
Solvent & Solubility
DMSO : 10 mg/mL (27.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 50 mg/mL (135.57 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. Cell viability of the drug-treated cells is normalized to their vehicle-treated controls, and the results are expressed as percentage viability. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compare with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Six-to 8-week-old male mice are injected s.c. with 107 low-passage human SUDHL-6, OCI-Ly7, or Toledo cells. Alternatively, 6-to 8-week-old mice are injected with low-passage HBL-1 cells. When tumors reach a palpable size (approximately 100 mm3), mice are assigned in a randomized way to treatment groups and treated i.p. with 25 or 50 mg/kg/d of the drugs (including FX1). Drugs are reconstituted in PEG-400 and stored at -20°C until use. Tumor size is measured 3 times a week with an electronic digital caliper in 2 dimensions, and then tumor volume is calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7113 mL | 13.5567 mL | 27.1135 mL | 67.7837 mL |
| 5 mM | 0.5423 mL | 2.7113 mL | 5.4227 mL | 13.5567 mL | |
| 10 mM | 0.2711 mL | 1.3557 mL | 2.7113 mL | 6.7784 mL | |
| 15 mM | 0.1808 mL | 0.9038 mL | 1.8076 mL | 4.5189 mL | |
| 20 mM | 0.1356 mL | 0.6778 mL | 1.3557 mL | 3.3892 mL | |
| 25 mM | 0.1085 mL | 0.5423 mL | 1.0845 mL | 2.7113 mL |