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A939572

Catalog No. T4515   CAS 1032229-33-6

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
A939572 Chemical Structure
A939572, CAS 1032229-33-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
2 mg In stock $ 57.00
5 mg In stock $ 87.00
10 mg In stock $ 117.00
25 mg In stock $ 243.00
50 mg In stock $ 477.00
100 mg In stock $ 683.00
500 mg In stock $ 1,390.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 100%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.
Targets&IC50 SCD1 (human):37 nM, SCD1 (mouse):<4 nM
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].
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].
Molecular Weight 387.86
Formula C20H22ClN3O3
CAS No. 1032229-33-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 56 mg/mL (144.38 mM)

TargetMolReferences and Literature

1. Roongta U V , Pabalan J G , Wang X , et al. Cancer Cell Dependence on Unsaturated Fatty Acids Implicates Stearoyl-CoA Desaturase as a Target for Cancer Therapy[J]. Molecular Cancer Research, 2011, 9(11):1551-1561. 2. Ben-David U , Gan Q F , Golan-Lev T , et al. Selective Elimination of Human Pluripotent Stem Cells by an Oleate Synthesis Inhibitor Discovered in a High-Throughput Screen[J]. Cell Stem Cell, 2013, 12(2):167-179. 3. Xin Z, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302.

TargetMolCitations

1. Liu Y, Wang Y, Lin Z, et al.SLC25A22 as a key mitochondrial transporter against ferroptosis by producing GSH and MUFAs.Antioxidants and Redox Signaling.2023 (ja). 2. Huang F, Zhao N, Cai P, et al.Active AKT2 stimulation of SREBP1/SCD1-mediated lipid metabolism boosts hepatosteatosis and cancer.Translational Research.2024

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Metabolism Compound Library Bioactive Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max Endoplasmic Reticulum Stress Compound Library Lipid Metabolism Compound Library Metabolism Compound Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library

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Keywords

A939572 1032229-33-6 Metabolism Dehydrogenase Stearoyl-CoA Desaturase (SCD) Inhibitor inhibit A-939572 A 939572 inhibitor

 

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