FX1
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MedKoo CAT#: 407501

CAS#: 1426138-42-2

Description: FX1 is an inhibitor of the B cell lymphoma 6 (BCL6). FX1 has 10-fold greater potency than endogenous corepressors and binds an essential region of the BCL6 lateral groove. 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. Low doses of FX1 induced regression of established tumors in mice bearing DLBCL xenografts. Furthermore, FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo.


Chemical Structure

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FX1
CAS# 1426138-42-2

Theoretical Analysis

MedKoo Cat#: 407501
Name: FX1
CAS#: 1426138-42-2
Chemical Formula: C14H9ClN2O4S2
Exact Mass: 367.97
Molecular Weight: 368.806
Elemental Analysis: C, 45.59; H, 2.46; Cl, 9.61; N, 7.60; O, 17.35; S, 17.39

Price and Availability

Size Price Availability Quantity
25mg USD 150 Ready to ship
100mg USD 250 Ready to ship
200mg USD 450 Ready to ship
500mg USD 950 Ready to ship
1g USD 1750 Ready to ship
2g USD 3250 Ready to ship
5g USD 4950 2 weeks
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Synonym: FX1; FX-1; FX 1.

IUPAC/Chemical Name: (5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid

InChi Key: VISHSGZPGQKEFX-KHPPLWFESA-N

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/h1-2,5H,3-4H2,(H,16,20)(H,18,19)/b11-10-

SMILES Code: O=C(O)CCN(C/1=O)C(SC1=C2C(NC3=C/2C=C(Cl)C=C3)=O)=S

Appearance: Red solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: FX1 is a BCL6 inhibitor with an IC50 of around 35 μM.
In vitro activity: To assess the capacity of FX1 to suppress DLBCLs (diffuse large B cell lymphomas), a panel of GCB-DLBCL cell lines (8 BCL6 dependent and 4 BCL6 independent) was treated with different concentrations of FX1 for 48 hours and the concentration of compound required to inhibit 50% of growth in comparison with vehicle-treated cells (GI50) was determined. FX1 showed a selective effect on BCL6-dependent DLBCLs with average GI50 values of about 36 μM, whereas GI50 values could not be determined in BCL6-independent DLBCLs, since they did not even reach 50% growth inhibition at concentrations of drug higher than 125 μM (Figure 4A). Reference: J Clin Invest. 2016 Sep 1;126(9):3351-62. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5004937/
In vivo activity: The survival rate of mice models of LPS-induced sepsis was improved in following FX1 administration. FX1 decreased the production of inflammatory cytokines, attenuated macrophage infiltration activities and reduced monocytes chemotaxis activities, all of which suggest that FX1 exert anti-inflammatory effects. Mechanistically, FX1 may enhance the affinity of BCL6 binding to downstream target pro-inflammatory genes. Reference: Int Immunopharmacol. 2019 Oct;75:105789. https://www.sciencedirect.com/science/article/pii/S1567576919301717?via%3Dihub

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.2 65.67
DMF 30.0 81.34

Preparing Stock Solutions

The following data is based on the product molecular weight 368.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Cardenas MG, Yu W, Beguelin W, Teater MR, Geng H, Goldstein RL, Oswald E, Hatzi K, Yang SN, Cohen J, Shaknovich R, Vanommeslaeghe K, Cheng H, Liang D, Cho HJ, Abbott J, Tam W, Du W, Leonard JP, Elemento O, Cerchietti L, Cierpicki T, Xue F, MacKerell AD Jr, Melnick AM. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep 1;126(9):3351-62. doi: 10.1172/JCI85795. Epub 2016 Aug 2. PMID: 27482887; PMCID: PMC5004937. 2. Zhang H, Qi X, Wu J, Huang X, Zhang A, Chen S, Ding X, Chen S, Le S, Zou Y, Xu H, Ye P, Xia J. BCL6 inhibitor FX1 attenuates inflammatory responses in murine sepsis through strengthening BCL6 binding affinity to downstream target gene promoters. Int Immunopharmacol. 2019 Oct;75:105789. doi: 10.1016/j.intimp.2019.105789. Epub 2019 Aug 8. PMID: 31401377.
In vitro protocol: 1. Cardenas MG, Yu W, Beguelin W, Teater MR, Geng H, Goldstein RL, Oswald E, Hatzi K, Yang SN, Cohen J, Shaknovich R, Vanommeslaeghe K, Cheng H, Liang D, Cho HJ, Abbott J, Tam W, Du W, Leonard JP, Elemento O, Cerchietti L, Cierpicki T, Xue F, MacKerell AD Jr, Melnick AM. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep 1;126(9):3351-62. doi: 10.1172/JCI85795. Epub 2016 Aug 2. PMID: 27482887; PMCID: PMC5004937.
In vivo protocol: 1. Zhang H, Qi X, Wu J, Huang X, Zhang A, Chen S, Ding X, Chen S, Le S, Zou Y, Xu H, Ye P, Xia J. BCL6 inhibitor FX1 attenuates inflammatory responses in murine sepsis through strengthening BCL6 binding affinity to downstream target gene promoters. Int Immunopharmacol. 2019 Oct;75:105789. doi: 10.1016/j.intimp.2019.105789. Epub 2019 Aug 8. PMID: 31401377.

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1: Cardenas MG, Yu W, Beguelin W, Teater MR, Geng H, Goldstein RL, Oswald E,
Hatzi K, Yang SN, Cohen J, Shaknovich R, Vanommeslaeghe K, Cheng H, Liang D, Cho
HJ, Abbott J, Tam W, Du W, Leonard JP, Elemento O, Cerchietti L, Cierpicki T, Xue
F, MacKerell AD Jr, Melnick AM. Rationally designed BCL6 inhibitors target
activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep
1;126(9):3351-62. doi: 10.1172/JCI85795. Epub 2016 Aug 2. PubMed PMID: 27482887;
PubMed Central PMCID: PMC5004937.