| Name | A939572 |
| Description | A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1. |
| Kinase Assay | Caki1 and A498 cells were transiently transfected with p5xATF6-GL3 UPR luciferase reporter and pRL-CMV-renilla luciferase plasmid using Lipofectamine2000 (Invitrogen). Cells (DMSO vs. A939572, NT vs. shSCD780) were harvested after 48hrs using Dual Luciferase assay kit per the manufacturer s protocol and luciferase activity was measured using a Veritas Luminometer; reported as relative luminescence[3]. |
| 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[3]. |
| 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[1][2]. |
| 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[3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (116.02 mM)
|
| Keywords | Inhibitor | inhibit | Stearoyl-CoA Desaturase (SCD) | A939572 | A-939572 | A 939572 |
| Inhibitors Related | Disulfiram | Methotrexate | ALDH1A3-IN-3 | Rotenone | Mycophenolate Mofetil | Ribavirin | 4-Diethylaminobenzaldehyde | Benzyl alcohol | Isomalt | Isoniazid | Sodium Oxamate | Ivosidenib |
| Related Compound Libraries | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Anti-Obesity Compound Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
