Art. -Nr.: HY-102027

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FX1

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

FX1 is a potent and specific BCL6 inhibitor, with an IC₅₀ of around 35 μM.

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Reinheit: 98.0%
CAS. Nr.: 1426138-42-2
Formel: C₁₄H₉ClN₂O₄S₂
Molecular Weight:368.82

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

FX1 Chemical Structure

CAS. Nr.: 1426138-42-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

FX1 is a potent and specific BCL6 inhibitor, with an IC₅₀ of around 35 μM.

IC₅₀ & Target

IC50: ~35 μM (BCL6)^[1]

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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.

In Vivo

Spleens in FX1-treating mice are macroscopically indistinguishable from vehicle controls. Total B cell abundance measured by flow cytometry is unaffected by FX1. GC B cells (GL7⁺FAS⁺B220⁺) are significantly depleted by exposure to FX1. Splenic architecture is examined by IHC. Staining with B220 antibody reveals normal B cell follicular structures, whereas staining for the GC B cell-specific marker peanut agglutinin shows profound loss of GCs. The half-life is estimated to be approximately 12 hours. Finally, whether FX1 can induce toxic effects in mice is assessed. 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 compare with vehicle^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1426138-42-2
Appearance Solid
Molecular Weight 368.82
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Working 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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 50 mg/mL (135.57 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mariano G et al. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep 1; 126(9): 3351–3362. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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FX1

Apoptosis Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) FX1

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FX1

Apoptosis Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) FX1

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FX1 Related Classifications

HY-102027 Related Classifications