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SML2074

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

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Size/SKUAvailabilityPrice
25 mg

Available to ship TODAYfromMILWAUKEE

$467.00
$396.95

About This Item

Empirical Formula (Hill Notation):
C14H9ClN2O4S2
CAS Number:
1426138-42-2
Molecular Weight:
368.82
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder

$396.95

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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

InChI key

VISHSGZPGQKEFX-KHPPLWFESA-N

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.).
Second generation 79-6 derived BCL6 inhibitor with improved efficacy against diffuse large B cell lymphoma (DLBCL) both in vitro and in vivo.

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This Item
X3629SML1735SML2688
FX1 ≥98% (HPLC)

Sigma-Aldrich

SML2074

FX1

X80 ≥98% (HPLC)

Sigma-Aldrich

X3629

X80

PFM01 ≥98% (HPLC)

Sigma-Aldrich

SML1735

PFM01

J30-8 ≥98% (HPLC)

Sigma-Aldrich

SML2688

J30-8

description

≥98% (HPLC)

description

≥98% (HPLC)

description

≥98% (HPLC)

description

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

color

red-brown

color

orange

color

white to beige

color

white to beige

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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."

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