SR-9243 Chemical Properties

Melting point:

154-155°C

Boiling point:

786.3±70.0 °C(Predicted)

Density 

1.347±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble in DMSO (greater than 25 mg/ml)

pka

-6.90±0.70(Predicted)

form 

solid

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Safety Information

HS Code 

29350090

SR-9243 Usage And Synthesis

Description

The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors. They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations. It reduces cancer cell viability (IC₅₀ values range from 15 to 104 nM) without cytotoxicity against non-malignant cells. SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.

Uses

SR9243 is used in new compounds targeting warburg effcts, killing cancer cells and inhibiting lipid production.

Definition

ChEBI: SR9243 is a sulfonamide resulting from the formal condensation of the sulfonic acid group of mesitylene-2-sulphonic acid with the amino group of 2-(m-bromophenyl)ethylamine in which the nitrogen is substituted by a 4-[m-(methylsulfonyl)phenyl]benzyl group. It has a role as an antineoplastic agent, an apoptosis inducer and a liver X receptor inverse agonist. It is a sulfonamide, a sulfone and a member of bromobenzenes.

storage

Store at +4°C

References

1) Flaveny?et al. (2015),?Broad anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis; Cancer Cell,?28?42

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