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FX1

Chemical Structure : FX1

CAS No.: 1426138-42-2

FX1 (BCL6 inhibitor FX1)

Catalog No.: PC-60927Not For Human Use, Lab Use Only.

FX1 (BCL6 inhibitor FX1) is a potent, specific BCL6 BTB domain inhibitor with Kd of 7 uM, binds with a greater affinity than the natural BCL6 ligand SMRT (Kd=30 uM).

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Biological Activity

FX1 (BCL6 inhibitor FX1) is a potent, specific BCL6 BTB domain inhibitor with Kd of 7 uM, binds with a greater affinity than the natural BCL6 ligand SMRT (Kd=30 uM).
FX1 exhibits 10-fold greater inhibitory activity against the BCL6 BTB domain in reporter assays with IC50 of 35 uM, displays good selectivity against a panel of 50 different kinases.
FX1 disrupts formation of the BCL6 repression complex, reactivates BCL6 target genes, suppresses ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo.

Physicochemical Properties

M.Wt 368.806
Formula C14H9ClN2O4S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mg/mL in DMSO

Chemical Name/SMILES

(Z)-3-(5-(5-chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid

References

1. Cardenas MG, et al. J Clin Invest. 2016 Sep 1;126(9):3351-62.

2. Deb D, et al. Cancer Res. 2017 Jun 1;77(11):3070-3081.

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