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

A939572 

Cat. No.: HY-50709 Purity: 98.77%
COA 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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
2 mg USD 72 In-stock
5 mg USD 108 In-stock
10 mg USD 144 In-stock
50 mg USD 576 In-stock
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200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 31 publication(s) in Google Scholar

A939572 Related Antibodies

Top Publications Citing Use of Products

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

    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 MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Mar;23(3):2064-2076.  [Abstract]

    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.

    A939572 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.  [Abstract]

    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 MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.  [Abstract]

    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 MedChemExpress. Usage Cited in: Oncogene. 2016 Jan 28;35(4):427-37.  [Abstract]

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

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • 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].

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

    A939572 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    387.86

    Appearance

    Solid

    Formula

    C20H22ClN3O3
    CAS No.
    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (257.82 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.98%

    COA (245 KB) LCMS (113 KB)

    Handling Instructions (2659 KB)
    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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    A939572 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    A9395721032229-33-6A 939572A-939572Stearoyl-CoA Desaturase (SCD)Inhibitorinhibitorinhibit

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