A BCL6 inhibitor (IC50 = ~35 μM); selective for BCL6 over a panel of 50 kinases at 10 μM; reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A

FX1 – 1 mg

Brand:
Cayman
CAS:
1426138-42-2
Storage:
-20
UN-No:
Non-Hazardous - /

FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6; IC50 = ~35 μM).{43297} 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, SUDLH-6, DOHH-2, OCI-Ly7, RCK8, SUDHL-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.  

 

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SKU: 23908 - 1 mg Category:

Description

A BCL6 inhibitor (IC50 = ~35 μM); selective for BCL6 over a panel of 50 kinases at 10 μM; reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A, CD69, and CXCR4 in a ChIP assay at 50 μM; represses growth of Farage, SUDLH-6, DOHH-2, OCI-Ly7, RCK8, SUDHL-4, OCI-Ly1, and SC-1 BCL6-dependent cell lines (GI50s = 16-54 μM); reduces tumor volume in an HBL-1 large B cell lymphoma mouse xenograft model at 50 mg/kg

Formal name: (5Z)-5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid

Synonyms: 

Molecular weight: 368.8

CAS: 1426138-42-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Transcription Factors

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