A BCL6 inhibitor
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FX1

Item No. 23908

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5Z)-5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid
CAS Number
1426138-42-2
Molecular Formula
C14H9ClN2O4S2
Formula Weight
368.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: slightly solublePBS (pH 7.2): slightly soluble
λmax
232, 276, 416 nm
SMILES
ClC1=CC=C2C(/C(C(N2)=O)=C3C(N(CCC(O)=O)C(S\3)=S)=O)=C1
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-
InChi Key
VISHSGZPGQKEFX-KHPPLWFESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Product Description

    FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6; IC50 = ~35 μM).1 It is selective for BCL6 over a panel of 50 kinases at a concentration of 10 μM. FX1 (50 μM) reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A, CD69, and CXCR4 in a ChIP assay. It represses growth of Farage, SU-DLH-6, DOHH-2, OCI-Ly7, RCK8, SU-DHL-4, OCI-Ly1, and SC-1 BCL6-dependent cell lines (GI50s = 16-54 μM) but not OCI-LY1-B50, Karpas 433, OCI-Ly19, or Toledo BCL6-independent cell lines (GI50s = >125 μM). In vivo, FX1 (50 mg/kg) reduces tumor volume in an HBL-1 large B cell lymphoma mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cardenas, M.G., Yu, W., Beguelin, W., et al. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma. J. Clin. Invest. 126(9), 3351-3362 (2016).