Skip to Content
Merck
All Photos(1)

Key Documents

SML2074

Sigma-Aldrich

FX1

≥98% (HPLC)

Synonym(s):

(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

Sign Into View Organizational & Contract Pricing

Select a Size

5 MG
£102.00
25 MG
£352.00

£102.00

Please contact Customer Service for Availability
Request a Bulk Order
All Photos(1)

Select a Size

Change View
5 MG
£102.00
25 MG
£352.00

About This Item

Empirical Formula (Hill Notation):
C14H9ClN2O4S2
CAS Number:
1426138-42-2
Molecular Weight:
368.82
UNSPSC Code:
12352200
NACRES:
NA.77

£102.00

Please contact Customer Service for Availability
Request a Bulk Order

Assay

≥98% (HPLC)

form

powder

color

red-brown

storage temp.

2-8°C

SMILES string

S1\C(=C2\c3c(ccc(c3)Cl)NC\2=O)\C(=O)N(C1=S)CCC(=O)O

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.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number
0000177507
0000177506

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Wendy Béguelin et al.
Cancer cell, 30(2), 197-213 (2016-08-10)
The EZH2 histone methyltransferase mediates the humoral immune response and drives lymphomagenesis through formation of bivalent chromatin domains at critical germinal center (GC) B cell promoters. Herein we show that the actions of EZH2 in driving GC formation and lymphoma
H S Madapura et al.
Oncogene, 36(32), 4619-4628 (2017-04-04)
B-cell CLL/lymphoma 6 (BCL6) exerts oncogenic effects in several human hematopoietic malignancies including chronic myeloid leukemia (CML), where BCL6 expression was shown to be essential for CML stem cell survival and self-renewal during imatinib mesylate (IM) treatment. As several lines
Mariano G Cardenas et al.
The Journal of clinical investigation, 126(9), 3351-3362 (2016-08-03)
Diffuse large B cell lymphomas (DLBCLs) arise from proliferating B cells transiting different stages of the germinal center reaction. In activated B cell DLBCLs (ABC-DLBCLs), a class of DLBCLs that respond poorly to current therapies, chromosomal translocations and amplification lead
William McCoull et al.
Journal of medicinal chemistry, 60(10), 4386-4402 (2017-05-10)
Inhibition of the protein-protein interaction between B-cell lymphoma 6 (BCL6) and corepressors has been implicated as a therapeutic target in diffuse large B-cell lymphoma (DLBCL) cancers and profiling of potent and selective BCL6 inhibitors are critical to test this hypothesis.

Questions

  1. What is the procedure for solubilizing or preparing product SML2074 for use or injection?

    1 answer

    1. We don't have an in-house protocol for the use of BCL6 Inhibitor, FX1 in vivo. However, there are relevant citations in the published literature. For example:

      - "Mice were assigned in a randomized way to treatment groups and treated i.p. with 25 or 50 mg/kg/d of the drugs. Drugs were reconstituted in PEG-400 and stored at –20°C until use."
      - "Mice were exposed to either vehicle (DMSO) or FX1 1 h prior to the LPS (10 mg/kg) challenge."
      - "Mice were injected i.p. with 50 mg/kg of compound in vehicle (35% PEG-300, 5% Tween-80, 65% Dextrose 5%, n=8) or vehicle alone (n=2)."

      Additional citations can be found by conducting a search for "inject BCL6 inhibitor FX1 mg/kg DMSO."

      Helpful?

Reviews

No rating value

Active Filters

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service