A939572

SKU: orb1302794

Description

A939572 is a potent and selective inhibitor of stearoyl-CoA desaturase 1 (SCD1), exhibiting IC50 values of <4 nM for murine and 37 nM for the human enzyme. This tool compound is widely used in metabolic disease and cancer research to investigate lipid metabolism in both cellular and animal models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1032229-33-6
• MW: 387.9
• Purity: >98%
• Formula: C₂₀H₂₂ClN₃O₃
• SMILES: CNC(=O)c1cccc(NC(=O)N2CCC(CC2)Oc2ccccc2Cl)c1
• Target: UPR (Unfolded protein response)
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• Target IC50:
  SCD1 (mouse):<4 nM |SCD1 (human):37 nM
• In Vivo:
  Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts were treated with A939572 and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) was recorded . A939572 and Tem monotherapy generated similar growth responses with approximately 20 30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yielded over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment. All of the animals maintained a healthy weight throughout the course of the treatment , however those in both the A939572 and the Combo group exhibited increased blinking, and slight mucosal discharge from the eyes after the first week of treatment.
• In Vitro:
  A939572 has been used to induce cell death of hPSCs as well as to inhibit the proliferation of human non-small cell lung carcinoma H1299 cells in vitro.
• Animal Research:
  A498 cells were subcutaneously implanted in athymic nu/nu mice at 1×10^6 cells/mouse in 50%Matrigel. Tumors reached ~50 mm^3 prior to 4wk treatment. A939572 was re-suspended in strawberry-flavored Kool-Aid in sterilized H2O (0.2g/mL) vehicle at 30mg/kg in a 50μl dose. Mice were orally fed by using a syringe to administer the 50μl dose twice daily/mouse. This modified method was found to be effective and less stressful on the mice. Temsirolimus was solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10mg/kg in a 50μl dose once every 72hrs/mouse. Tumor volumes were calculated using the formula and body weight were measured every 3 days.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

A939572, A-939572, A 939572, inhibit, Inhibitor, SCD, SCD1 (human), SCD1 (mouse), Stearoyl-CoA Desaturase, StearoylCoA Desaturase (SCD), StearoylCoADesaturase(SCD), Stearoyl-CoA Desaturase (SCD), StearoylCoADesaturase

Compound Identifiers

PubChem CID

24905400