1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. A939572

A939572 

Cat. No.: HY-50709 Purity: 99.67%
Handling Instructions

A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.

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

A939572 Chemical Structure

A939572 Chemical Structure

CAS No. : 1032229-33-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
2 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A939572 purchased from MCE. Usage Cited in: Oncogene. 2016 Jan 28;35(4):427-37.

    HeLa cells are treated with vehicle (DMSO) or 200 nM SCD-1 inhibitor for 40 h after which cells are analysed via TEM.

    A939572 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.

    Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in T98G-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

    A939572 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.

    Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in U87-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

    A939572 purchased from MCE. Usage Cited in: J Cell Mol Med. 2019 Mar;23(3):2064-2076.

    Cyclins D1, Rb, PCNA, Cdk4 and Cdk6 are down-regulated after either 24 h treatment of A939572 or siRNAs, while cyclin E1 is up-regulated.

    A939572 purchased from MCE. Usage Cited in: J Cell Mol Med. 2019 Mar;23(3):2064-2076.

    Compared to the DMSO (0.25%) group, A939572 at concentrations of 6.4 and 12.8 μg/mL up-regulate E-cadherin expression and down-regulate N-cadherin expression.
    • Biological Activity

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    • Customer Review

    Description

    A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.

    IC50 & Target

    IC50: <4 nM (mSCD1), 37 nM (hSCD1)[1]

    In Vitro

    A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects[1]. A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC50s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi) treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA-BSA[2].

    In Vivo

    Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) is recorded. A939572 and Tem monotherapy generate 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 yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment[2].

    Molecular Weight

    387.86

    Formula

    C₂₀H₂₂ClN₃O₃

    CAS No.

    1032229-33-6

    SMILES

    O=C(N1CCC(OC2=C(Cl)C=CC=C2)CC1)NC3=CC=CC(C(NC)=O)=C3

    Shipping

    Room temperature in continental US; may vary elsewhere

    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 : ≥ 56 mg/mL (144.38 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5782 mL 12.8912 mL 25.7825 mL
    5 mM 0.5156 mL 2.5782 mL 5.1565 mL
    10 mM 0.2578 mL 1.2891 mL 2.5782 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    Cells are plated (0.5 or 1×105/well) in 24-well plates in triplicate. Cells are counted using a Coulter Particle Counter. Oleic acid-albumin is added to media at 5μMol. A939572 stocks are prepared in DMSO. Temsirolimus dosing is performed. Soft agar cultures are prepared by diluting 2× growth medium 1:1 in 1.5% Seaplaque®GTG® agarose, with 500 cells/plate in 60mm culture dishes. Colonies are stained with Giemsa and counted after 3wks[2].

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

    Animal Administration
    [2]

    Mice[2]
    A498 cells are subcutaneously implanted in athymic nu/nu mice at 1×106 cells/mouse in 50% Matrigel. Tumors reach ~50 mm3 prior to 4 wk treatment. A939572 is re-suspended in strawberry flavored Kool-Aid® in sterilized H2O (0.2 g/mL) vehicle at 30 mg/kg in a 50 μL dose. Mice are orally fed by using a syringe to administer the 50 μL dose twice daily/mouse. This modified method is found to be effective and less stressful on the mice. Temsirolimus is solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10 mg/kg in a 50 μL dose once every 72 hrs/mouse. Tumor volumes are calculated using the formula 0.5236 (L*W*H) and body weight are measured every 3 days.

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

    References
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