1. Metabolic Enzyme/Protease
  2. LXR
  3. SR9243

SR9243 

Cat. No.: HY-16972 Purity: 96.64%
Handling Instructions

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

For research use only. We do not sell to patients.

SR9243 Chemical Structure

SR9243 Chemical Structure

CAS No. : 1613028-81-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 65 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg USD 740 In-stock
Estimated Time of Arrival: December 31
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Description

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

In Vitro

SR9243 specifically targets LXR and downregulates LXR-mediated gene expression, dose-dependently suppresses LXRα- and LXRβ-dependent transcription at nanomolar concentrations, and potently inhibits LXR-driven luciferase activity in cultured cancer cells. SR9243 potently reduces cancer cell viability at nanomolar concentrations (IC50 appr 15-104 nM) in prostate (PC3 and!DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. And the colony-forming capacity of cancer cells is also significantly loared by SR9243 in a dose-dependent manner. SR9243 is a potent inhibitor of lipogenic gene expression that selectively kills cancer cells by depleting intracellular lipids. Combination of cancer cell media with oleate, stearate, and palmitate in combination completely rescues cancer cell viability in cancer cells. Fatty acid supplementation also rescues the viability of SW620 cells in which glycolysis is substantially disrupted[1].

In Vivo

SR9243 is able to profoundly inhibit tumor glycolysis, lipogenesis, and induce apoptotic cancer cell death without promoting weight loss in vivo. SR9243 inhibits tumor growth without profoundly repressing glycolytic gene expression, and inhibits tumor growth and lipogenesis without hepatotoxicity or inflammation in vivo[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (31.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5959 mL 7.9793 mL 15.9586 mL
5 mM 0.3192 mL 1.5959 mL 3.1917 mL
10 mM 0.1596 mL 0.7979 mL 1.5959 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cancer cells are plated at low-density (5×103) cells per well. Cells are then treated with either DMSO vehicle control, SR9243 (100 nM) or SR9243 (10 μM) and allowed to grow for 4 days. Colonies are then fixed with Formaldehyde (1%) and stained with Crystal violet solution (0.05% w/v)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
C57BL/6J, Nu/Nu and Ob/Ob mice are used in the assay. Mice are housed in sterile ventilated cages, fed a standard diet, and provided water ad libitum. Mice are treated after two weeks of acclimation. Mice are monitored daily for signs of illness, pain, or severe weight loss. All mice are humanely euthanized using CO2 followed by cervical dislocation. For liver lipid content analysis 8-week old male Ob/Ob mice are fed a high fat diet (60% kcal/fat, 20% carbohydrate) for the duration of the experiment and are treated with vehicle or SR9243 for 3 days. Mice are injected (i.p.) with either vehicle (10% DMSO, 10% Tween-80) or SR9243 (30 mg/kg) once daily[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

626.62

Formula

C₃₁H₃₂BrNO₄S₂

CAS No.

1613028-81-1

SMILES

BrC1=CC(CCN(S(C2=C(C)C=C(C)C=C2C)(=O)=O)CC(C=C3)=CC=C3C4=CC(S(=O)(C)=O)=CC=C4)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere

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SR9243
Cat. No.:
HY-16972
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SR9243

Cat. No.: HY-16972