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SML2074 Sigma-Aldrich

FX1

≥98% (HPLC)

Synonym: (5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid, (Z)-3-(5-(5-Chloro-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid

  • CAS Number 1426138-42-2

  • Empirical Formula (Hill Notation) C14H9ClN2O4S2

  • Molecular Weight 368.82

  •  NACRES NA.77

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, F
assay   ≥98% (HPLC)
form   powder
color   red-brown
storage temp.   2-8°C

Description

Biochem/physiol Actions

FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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